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GABAB receptor

G-protein coupled receptor

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  • 3 chapters

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The receptors were first named in 1981 when their distribution in the CNS which was determined by Norman Bowery and his team using radioactively labelled baclofen.

Functions

GABABRs stimulate the opening of K+ channels, specifically GIRKs, which brings the neuron closer to the equilibrium potential of K+. This reduces the frequency of action potentials which reduces neurotransmitter release. Thus GABAB receptors are usually considered as inhibitory receptors.

GABAB receptors can also function as an excitatory receptor and facilitate neurotransmitter release via increasing the activity of CaV2.3 channels.

GABAB receptors usually reduces the activity of adenylyl cyclase and Ca2+ channels by using G-proteins with Gi/G0 α subunits.

GABAB receptors are involved in behavioral actions of ethanol, gamma-hydroxybutyric acid (GHB), baclofen, and possibly in pain. Recent research suggests that these receptors may play an important developmental role.

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