Agonists
Full agonists
• If a drug binds to receptor and
produces a maximal biologic
response that mimics the response
of endogenous ligand, it’s full
agonist.
• 100% efficacy
• Depends upon concentration
• Has much high higher affinity for
active receptor than Ri receptor
confirmation.
• Intrinsic activity = 1
e.g., phenylephrine is full agonist at
alpha-adrenoceptors.
Pharmacological antagonists
A drug binds to the same receptor as
the agonist does.
1. Competitive antagonists:
( terazosin competes with
norepinephrine at alpha –
adrenoceptors )
2. Non-competitive antagonists:
(phenoxybenzamine and
norepinephrine)
Partial agonists
• If a drug binds to a receptor and
can’t produce same Emax even
when all the receptors are occupied
then it’s partial agonist.
• Less than 100% efficacy
• Independent from concentration
• In the presence of full agonist,a
partial agonist may act as a partial
antagonist.
• Intrinsic activity =greater than zero
but less than 1
e.g., aripipraxole is partial antagonist
at selected dopamine receptors
Antagonists
Physiological antagonists
Agonist and antagonist bind
with different receptors of the
same physiological system and
produce opposite effects.
e.g., NE >>
bronchoconstriction while
Histamine>>bronchodilation
Inverse agonists
• Binds much more rapidly to Ri
receptor confirmation, prevent
conversion to Ra state and reduces
the constitutive activity.
• Intrinsic activity = less than
Chemical antagonists
Agonist and antagonist binds
with each other forming
agonist –antagonist complex
irrespective of binding to
receptor and produce inactive
product.
e.g., pralidoxime is a chemical
antagonist of
organophosphate