Lecture 4 - Nature of Drug Targets Flashcards
1
Q
Most small molecule drugs target…
A
receptors, (GPCR), ions channels.
2
Q
Agonist
A
mimics activity of endogenous ligand
3
Q
Antagonist
A
blocks effect (binding) of endogenous ligand
4
Q
Partial Agonist
A
mimics activity but plateaus at lower levels
5
Q
Inverse Agonist
A
has opposite activity of agonist
6
Q
Methadone
A
full agonist on opioid receptor
7
Q
Buprenorphine
A
more potent but only partial agonist so is less “efficacious”
8
Q
Naloxone
A
competitive antagonist & blocks effects of both agonists & partial agonists
9
Q
Competitive antagonists
A
shift activity curve of agonist to right. Takes more of agonist to give full effect.
10
Q
Noncompetitive antagonists
A
affect both binding & activity & prevent agonist from achieving full effect
