GABA receptor activation

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R-HSA-977443
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Homo sapiens
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Gamma aminobutyric acid (GABA) receptors are the major inhibitory receptors in human synapses. They are of two types. GABA A receptors are fast-acting ligand gated chloride ion channels that mediate membrane depolarization and thus inhibit neurotransmitter release (G Michels et al Crit Rev Biochem Mol Biol 42, 2007, 3-14). GABA B receptors are slow acting metabotropic Gprotein coupled receptors that act via the inhibitory action of their Galpha/Go subunits on adenylate cyclase to attenuate the actions of PKA. In addition, their Gbeta/gamma subunits interact directly with N and P/Q Ca2+ channels to decrease the release of Ca2+. GABA B receptors also interact with Kir3 K+ channels and increase the influx of K+, leading to cell membrane hyperpolarization and inhibition of channels such as NMDA receptors (A Pinard et al Adv Pharmacol, 58, 2010, 231-55).

Literature References
PubMed ID Title Journal Year
17364682 GABAA receptors: properties and trafficking

Michels, G, Moss, SJ

Crit Rev Biochem Mol Biol 2007
20655481 GABAB receptor coupling to G-proteins and ion channels

Padgett, CL, Slesinger, PA

Adv Pharmacol 2010
15269338 Molecular structure and physiological functions of GABA(B) receptors

Bettler, B, Kaupmann, K, Mosbacher, J, Gassmann, M

Physiol Rev 2004
11283747 Constructing inhibitory synapses

Moss, SJ, Smart, TG

Nat Rev Neurosci 2001
20655485 GABAB receptors: physiological functions and mechanisms of diversity

Pinard, A, Seddik, R, Bettler, B

Adv Pharmacol 2010
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