Flashcards in Receptors Deck (18)
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1
affinity =
potency
2
tendency to activate a receptor =
efficacy
3
antagonists and efficacy =
antagonists have 0 efficacy (when neutral)
4
a partial agonist and efficacy
partial agonists have an intermediate level of efficacy.so even at 100% binding to receptors, they can only produce an intermediate effect
5
efficacy describes
the tendency of the drug-receptor complex to adopt the active AR* rather than the resting AR state.
A drug with 0 efficacy has no tendency to cause receptor activation and causes no tissue response.
6
muscarinic actylcholine receptors
adrenoreceptors
GPCR
7
nicotinic acetylcholine receptor
GABA
Ligand gated
8
fast transmission is associated with
ligand gated channels
9
cys-loop receptor subunits
five subunits !!
10
inotropic glutmate receptor subunits
four !!
11
Examples of cys-loop receptors
nicotinic acteylcholine receptor, glycine receptor, 5ht-3receptor
12
Examples of inotropic glutamate receptors
AMPA receptor
NMDA receptor
kaintate receptor
13
gating on a cys-loop receptor
the second transmembrane domain of the subunit generally obstructs the pore
14
cys-loop receptor has two
alpha sub units
15
Drugs that act on cys-loop receptors
Nicotine/Chantix (nACH)
Ambien, barbiturates, ETOH -> GABAa
16
drugs that act on inotropic glutamate receptors
Ketamine (NMDA)
Aniracetam (AMPA)
17
Special properties that underly NMDA receptor involvement in LTP
VG magnesium block, permeability to Ca2+
18
