lecture 4 Flashcards
antagonist
no intrinsic activity (when bound to receptor, nothing happens), inhibitor
agonist
intrinsic activity, activator, receptor affinity
partial agonist
blocks other agonists
ACh
causes reduction in blood pressure
competitive antagonism
more of sort wins, antagonist reduces potency of agonist without affecting the agonist efficacy, curve moves to the right because the concentration increases.
noncompetitive antagonism
antagonist reduces the efficacy of an agonist, changes the maximum and curve moves a bit to the right.
functional antagonism
have a function, two agonist induce an opposite effect via activation of different receptors
B1
stimulates heart rate
M3, B2
Lung
M2, B1
Heart
GPCR’s activate their effect system via…
Ga and Gby subunits
Gi
inhibits
Gs
stimulates
Forskolin
direct stimulation of AC without receptor activation
Theophylline
inhibition of cAMP-specific phosphodiesterase