Neurotransmitter Systems II: GABA And Glycine Flashcards
What does GABA stand for?
Gamma-aminobutyric acid
What is GABA?
Major inhibitory neurotransmitter in the CNS
What is the main precursor to GABA?
Glucose
How does glucose turn into GABA?
Glucose -> glutamate, which then is turned into GABA by glutamate decarboxylase with the cofactor pyridoxal phosphatase
What shaped vesicles is glutamate stored in?
Round
What shaped vesicles is GABA stored in
Oval
How is GABA retaken up?
High affinity sodium dependant GABA transporters GAT-1 on neurons and GAT-3 on glial cells
What are the steps in GABA degredation (no enzymes)?
GABA -> succinic semialdehyde -> succinic acid
What enzyme catalyses GABA -> succinic semialdehyde?
GABA Transaminase (GABA-T)
What enzyme catalyses succinic semialdehyde -> succinic acid?
Succinic semialdehyde dehydrogenase (SSADH)
What type of receptors are GABAa receptors?
Ionotropic
What type of receptors are GABAb receptors?
Metabotropic
What happens upon GABA binding to GABAa receptor?
Channel opens and allows the influx of chloride ions
What are the possible GABAa receptor subunits?
6 alpha, 3 beta, 3 gamma, delta, epsilon, pi and theta
What is the most common GABAa configuration?
2 alpha, 2 beta and a gamma
Why are GABAa receptors a key drug target?
Multiple binding sites
Where do agonists/ antagonists bind on GABAa receptors?
Between the alpha and beta subunits
Where does benzodiazepine bind on GABAa receptors?
Between alpha and gamma subunits
Where do channel blockers bind on GABAa receptors?
Blocks the ion pore (non-competitive antagonist)
How do channel modulators work on GABAa receptors?
Increase the opening