site 2 acetylation oral antagonist cAMP adenylyl cyclase hydrogen bond second messenger prodrug increases unionized van der waals selectivity stereoisomers acceptor TD50 site 3 individual reduced targets indirect agonist hydroxyl group hydrophilic lipophilic hydrolysis affinity ionic bond absorption efficacy hydroxylation isosteres pharmacokinetic partial agonist phase I decreases ED50 phase II down regulation population ionized spare receptors enzyme inducer pharmacodynamic site 2 acetylation oral antagonist cAMP adenylyl cyclase hydrogen bond second messenger prodrug increases unionized van der waals selectivity stereoisomers acceptor TD50 site 3 individual reduced targets indirect agonist hydroxyl group hydrophilic lipophilic hydrolysis affinity ionic bond absorption efficacy hydroxylation isosteres pharmacokinetic partial agonist phase I decreases ED50 phase II down regulation population ionized spare receptors enzyme inducer pharmacodynamic
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site 2
acetylation
oral
antagonist
cAMP
adenylyl cyclase
hydrogen bond
second messenger
prodrug
increases
unionized
van der waals
selectivity
stereoisomers
acceptor
TD50
site 3
individual
reduced
targets
indirect agonist
hydroxyl group
hydrophilic
lipophilic
hydrolysis
affinity
ionic bond
absorption
efficacy
hydroxylation
isosteres
pharmacokinetic
partial agonist
phase I
decreases
ED50
phase II
down regulation
population
ionized
spare receptors
enzyme inducer
pharmacodynamic