        

 








        

   
 

         


           
















          





      
 
        



        




         

         
         


         

 

 






 

 
  
 


         
           

         
          


          
      
         

      



























          



          
        
        













        
        



      
      
  


   
      



        
       


        
     
      
       


       
 
         

        



 

 



  
         
        




     
 

 
  
        


         










           




    





    
         



  
         
         





      







         





         



    



















         

          



       







          

  



 
       
 




          


















          
      
        
        
         





         


        

        






    




       
   
        

  

        
         



          

      

 




          




         

        


        
            

            



          

 
          


     



          

 

        

    

        

          

 












      


           


 


 
 
  
          









 


 

  
         


          
         

          











        




    



       

       



       

       
       



        
   





      





   
        





       












         


         

        


         
 













 





  




         
         



    
 

  





     


        

 






 


   
         
















 
         



g 
g

            



          



 
 
        
    


        




 







  


 




 



 




  
  


  

 

 
 




 
 
 
          
         








 
 
    

       

 

  
 
 
 
  
 
  

 
 


 




       
         




       





 





 








        


  
          





        




  





        

          




        







        
   
           
          



       

















           

 


        








 





 







         
      



         

 


   





 

          
            
 

 







 
 
 




      










       


 





 





        






  

   





        
         
















  


   



 






         
 

 


 
        

        

          

        



      


 

       

          
          
           





 


        
           





  


 


 



   


              


 
          
   

          
 
 
           

  







       





   
       
       





        
       














 

 



        
  

         
        




          
        
       






 


    



      
 
         

 


     


        







   

 
 

      






        



 
        
 
          





         
          

 
          



       




        








       
    




        






         





         
         




        


         
 
           
 


   

  
          

  
 
 b
   
        




         





         



           


          






        










       



        
 

         

         

      





          









        
      

       







           






 






 

 







   
      








       







 









    
        

       










 


    espuesta  

        
         
       
         
        
         
       


  


   
  D      
   

  








  
 
   

 A   
  
   
   A      D
       








 
        
  





         




 



     
      








       









         

     
      


          
 


 

 


         




  
        
       

  
          










 
 


       
        





        Surge antagonismo competitivo cuando el agonista A y el antagonista I
compiten por el mismo sitio de unión en el receptor. Las curvas de respuesta correspondientes al agonista se desplazan a la derecha, por un
mecanismo que depende de la concentración, por parte del antagonista, de modo que EC50 del agonista aumenta (p. ej., L contra L , L y L )
con la concentración del antagonista.  Si el antagonista se liga al mismo sitio que el agonista pero lo hace de manera irreversible o seudo-
irreversible (disociación lenta sin enlace covalente), originará un desplazamiento de la curva de dosis-respuesta a la derecha, con disminución
mayor de la respuesta máxima. Los efectos alostéricos surgen cuando el ligando I se une a un sitio diferente en el receptor, para inhibir la
respuesta    o potenciarla    Dicho efecto es saturable; la inhibición llega a un valor “limitante” cuando hay
ocupación completa del sitio alostérico.
        


       
         


          
          





  
 
      



           
 
       
 
     
 



 
 
  
 

 
 
 
 
 


 
   
  
  
    
 
D    



 
   
   
       
         

          
 
             
  
 
    
      
  
    
      
 

          

  
     
  




 





        
         
   




        













          


 


         




          
 


     

           
      

       
 





 

   

 

        
      
  

  

        
 

          
  


  

  
        
       
        
  


 




 

 
        
 

         




 
 
  


 


  

  

  

  

  
  

       
  

  


 