GABA ☺️ Flashcards
Describe the distribution and the characteristics of GABA
Widely distributed in CNS (30% of synapses)
Very little in PNS
AA
MOST IMPORTANT INHIBITORY NT IN CNS
Describe the synthesis of GABA
Glutamate =(GAD)=> GABA
Describe the storage of GABA
vGABAT (GABA 2H exchanger)
-H gradient driven by HATPase
Describe the release of GABA
Ca dependent vesicular release at axon terminal
Describe the receptors that respond to
GABA
-what drugs are clinically useful
-what are they used for
Ionotropic GABAa receptor anion channel
-Cl entry
Metabotropic GABAb to Gi, o
GABAa - benzodiazapine (agonist), propofol (anaesthetic)
GABAb - baclofen (agonist for alcohol withdrawal)
Describe the reuptake of GABA
- what drugs are clinically useful
- what are they used for
GAT symport with Na into neurone or glia
Tiagabine (blocks GAT to treat epilepsy)
Describe the degradation of GABA
- what drugs are clinically useful
- what are they use for
Mainly occurs in glia
GABA =(GABA transaminase)=> succinic semialdehyde
GABA transaminase also converts a oxoglutarate to glutamate
Vigabatrine (blocks GABAt in epilepsy treatment)
What recreational drugs affect the GABA pathway
-could they be used clinically?
Barbiturates = anticonvulsant, sedatives NO = analgesic
How would you manage these conditions that are affected by the GABA pathway
- epilepsy
- anxiety
- insomnia
- muscle tone
Epilepsy => not enough GABA
Anxiety =>
-GABA agonists could be used as a sedative
Insomina => GABA can be used as a sedative
Muscle tone => GABA agonists can be used as muscle relaxants
GABA critical for CNS function