GABA Flashcards
GABAaR is what kind of channel
transmitter gated anion channel
GABAbR is what kind of receptor
G protein coupled receptor
Drugs that enhance the GABAaR are called what
positive allosteric modulators
what are positive allosteric modulators
drugs that enhance GABAaR function
What kind of dimer is GABAbR
heterodimer
What are the 2 alphas on the GABAbR
alphai
alphaO
name a selective GABAbR agonist
baclofen
what is baclofen
GABAbR agonist
why is baclofen administered to patients
treat certain types of spasticity
how is alpha - ketoglutarate converted to glutamate
GABA T
how is glutamate converted to GABA
Glutamic acid decarboxylase
activation of glutamate gated cation conducting channels produce what?
excitatory postsynaptic potential (EPSP)
activation of GABA-gated anion conducting channels produce what
inhibitory post synaptic potential (IPSP)
the firing of the pyramidal neuron causes what
activates an inhibitory interneuron
once the inhibitory interneuron is activated what does it inhibit
the pyramidal neuron
when can the pyramidal neuron start to fire again
once the inhibition has decayed
What does the Gi alpha subunit inhibit
adenylate cyclase
once the Gi alpha subunit has inhibited adenylate cyclase what does this decrease
cAMP levels
postsynaptic GABAb activation causes the Gi betagamma complex to open what
what will this cause
a K+ channel
hyperpolarisation
presynaptic GABAb activation causes the Go betagamma to decrease what
and what does this decrease
voltage gated Ca2+ channels opening
decreasing quantal release of neurotransmitter
GABA acts post-synaptically to activate what
what does this produce
chloride conducting GABAaRs
produces IPSP
GABA acts pre synaptically to activate what
what does this reduce the probability of
GABAbRs
reduces the probability of Ca2+ channel opening and consequently decrease GABA release upon a second stimulus
Drugs that inhibit GABAaR function are
pro convulsant
anciogenic
benziodiazepines ______ the probability of the channel opening
increases
barbituates ____ channel open states of long duration
promote
barbituates at higher concentrations directly ______ the receptor
activate
which alpha subunits does diazepam enhance and which does it not
alpha 1,2,3,5
not -> alpha 4
what is an agonist of GABAb
baclofen
what is an antagonist of GABAb
saclofen
