PHAR 562 Lecture Notes - Lecture 6: Clonazepam, Baclofen, Chemical Synapse
15 Oct 2017
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Document Summary
Gaba receptors and their synapses: genes, subtypes and activation mechanisms. Molecular identity: many distinct subunits with many possible combinations, mature receptors assemble as pentamers, gaba-ars are benzo sensitive or insensitive, found throughout the cns, gaba-rho aka gaba-c found in the retina. Acetylcholine receptors are pentamers, lysine receptors are pentamers, one of the first major genes cloned were for gaba receptors which are also pentamers. Gabar: the signaling mediated by gabar in synapse is called phasic signaling, the signaling outside the synapse is non-phasic or extrasynaptic signaling by gabar (tonic signaling) Activation mechanism: agonists and modulators bind at subunit interfaces, full-length structures of prokaryotic elic/glic as well as human gaba-ar, agonist efficacy may involve flipped/pre-gating states. Gaba a receptors are members of the cys-loop superfamily. There is a whole bunch of gabar genes: alpha: 6, gamma: 3, epsilon: 1, beta: 4, rho: 3, delta: 1, pi: 1. The number of potential gabar you can assemble from these subunits is enormous.
