Raney , ~ . 4 Dig al, 8 MMi dees ht se Whal a druq does to a oe A When a dtvq es to the body, ik then starts inte- yacting with cell receptors which in turn Seads be a formation of agnal and bhis signal bb a ene yeac ions PlGmntela results 7 SOE vidlo gical effect © Giana can rel) DNA to stop replicating- Cells Fferent receptors which unique *¢ Sponses: p £ wn our body ipve 0 Ne of ai when TcAMP feamp — TeAMP 3- ENZYME LINKED RECEPTORS ” On A ad receptor just G- se receptor have extracdular binding sites where the Viganel typically Harmone or a growth factor can attach and this stimulates ero numa et nside the cebl- Most enzyme linked receptors are Tursine kina type which Simply mean Rhey display Kinase ackue os and the amino acid “his “Tyrosine involved in Uhat- So the way they works is when Sigane binds to 2 of theereceplors, it causes Grrnational change Unat results in aggregation of both hese receptors- One the dimer is formed, Tyrosine odnes om activated and causes PIP to become fOP in autophosphorylation of the receptors. cine fixed up with Phosphate qroup, » dif fer- ms come up and attach themselves to Tyrosine This in turn causes confirmational ched protein ultimatdy Seading to ati Hat produces celular response SS, in ae - ea ~ , Mavary (blulaw Raper ing 6 5 9 ¢w . 4. INTRACELLULAR RESPONSE " We ; : pinside is receptor is Yocatecl entirely eh aatl. vata tae on cell membrane Therefore, the” Ligand has 1st bo cross the Lipid membrane and once inside the cell, it then binds to the veceptor Now the activated Vigand receptor complex Can move into the nucleus, bind to DNA & reqplate gene expression ullimatdy leading to the synthesis of specific Ligand Ba proteins Ce Memo sane "LIFE CYCLE OF RECEPTORS” Pray ise DNA contains code which is used bo synthesize sp sae from clifferent receptor assemble , Ona avemble Ure receptors get embedded into the cell, membrane and tan recieve & a rnotecuile ; % df calf recieves foo much lation which can potent- i Ces have ability to down ialty damage the cell, © a ae — receptors meaning they can @ cecycle them ubich Yeads to few sand thus decreased sensitivity response bo sign [ skime! sequlate Khe membrane and member express vec epro a signal molecules } es ae Care? DNA aheas cell receptors _ Gost and cell veci ewe abi fity to uprequiate tha receptors ct inserted on cal sensitivity to signal most of the signal, cells more x OF very weak which means hos increasing Example Signal molecule is of a drug . As comcentvation of Aroq pharmacological effect also increases until it all the receptors ar occ ied - receptors ! membrane molecwles actually a some kind increases , its reach the pant where Sf we plot this, we cletermine ECSO From the graph €CSO. os simply the concentration of a 21a of the maxiroum effect GME nat produces So] tells us how the potent oq 1S Dwg whch nas Vouwes ECSO is more potent Because Ness drug is needed bo get half of the max response Drvq ® also reach the same Devel of pharmacaleqical effect as ang Q-And this is due fo its EFFICACY - 4 ts Ae presented by So maximum efficacy of each dru which all the receptors are occupied by the don't produce larger effect potent but also move effi- Emax at dog and high concentration Dug As nok only more caci ow in the diagram ‘ i _"_—E—E rrr400}: Graph dose response MAX Phavmarelogical a8 Sciik —— | efficacy - “neTRINSIC ACTWITY © hte PES eemcaaaees activity refers to, the ability of the chug & Sout a drug binds to the maximal effect our bod- Jnbinsic produce marimal effect and vt is able produce receptors that is compavakle to the effect produced ou ies on endogenous Vigand - We called wo FOU | AGONIST’ oP ok ue veceptors chow some Kind=eols: the aaa «ky when, thee 15 no agonist around This is called BASAL ACWWITY a Sn presence eli Fol agonist , wonee Boe een effect PARATIAL AGONIST: The agonist that ts unable to pro: due maximal effect even if ik occupies all the receptors: IAWERSE AGONIST: the agent that binds to the veceptors, | inskeack of activating trem, ak stabilizes veceptors 19 ahi inactive form We called & inverse agonist - Because at snap ‘iminales barat activi l g i 1}. CBS gonist Pastiay 9 ical ae eae ee AS“ANTAGONIST” Aaa , On the other side of the spechum, we have anta ote which refers to a Viganel that can bind to the Compchtive 3 4 Pawn antagonist > Agonist + Competit- Biologic we antagonist effeck “3 tt oP Agonist + drreversible : antagonist FcsO £CSO (Agonist ) 04 Phenoxybenram ine Ana? advencdine ark aw adsenegic «cceplo's': 4 o : “ALLOSTERIC ANTAGONISTS ” “These bind to the ske different from agonist bindin vespont fo of Population 2