Receptors Flashcards
(18 cards)
affinity =
potency
tendency to activate a receptor =
efficacy
antagonists and efficacy =
antagonists have 0 efficacy (when neutral)
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
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.
muscarinic actylcholine receptors
adrenoreceptors
GPCR
nicotinic acetylcholine receptor
GABA
Ligand gated
fast transmission is associated with
ligand gated channels
cys-loop receptor subunits
five subunits !!
inotropic glutmate receptor subunits
four !!
Examples of cys-loop receptors
nicotinic acteylcholine receptor, glycine receptor, 5ht-3receptor
Examples of inotropic glutamate receptors
AMPA receptor
NMDA receptor
kaintate receptor
gating on a cys-loop receptor
the second transmembrane domain of the subunit generally obstructs the pore
cys-loop receptor has two
alpha sub units
Drugs that act on cys-loop receptors
Nicotine/Chantix (nACH)
Ambien, barbiturates, ETOH -> GABAa
drugs that act on inotropic glutamate receptors
Ketamine (NMDA)
Aniracetam (AMPA)
Special properties that underly NMDA receptor involvement in LTP
VG magnesium block, permeability to Ca2+
most common target for pharmacetuicals
GPCR
