GABAB receptors (GABABR) are metabotropic transmembrane receptors of gamma-aminobutyric acid (GABA), which were first identified in 1981 when their distribution in the CNS was determined. It is linked by G-proteins to potassium channels. These receptors are present in autonomic divisions of the central and peripheral nervous systems. The changing potassium concentrations hyperpolarize the cell at the end of an action potential. They stimulate the opening of K+ channels and bring the neuron closer to the equilibrium potential of K+. This reduces the frequency of action potentials that reduces the release of neurotransmitter. Therefore, GABAB receptors are inhibitory receptors. The reversal potential of the GABAB-mediated IPSP is approximately 100 mV, which is more hyperpolarized than the GABAA IPSP. GABAB receptors also reduce the activity of adenylyl cyclase and Ca2+ channels by using G-proteins with Gi/G0 α subunits. The receptors are involved in the action of gamma-hydroxybutyrate, ethanol, and may cause pain. Recent research suggests that GABAB receptors may play an important developmental role.
Fig.1 Colour confocal laser scanning images showing double-labeled neurons in the human striatum double-labeled for GABAB(1)(A) and GABAAα1(B) and the merged images (C). (Emson, 2007)
The actions of g-aminobutyrate (GABA) in the basal ganglia and throughout the mammalian CNS are mediated by two classes of GABA receptors, the GABAA and GABAB receptors. The GABAB receptor, in contrast to the GABAA channel, is coupled to G-proteins and is a metabotropic receptor. A number of groups established that the functional GABAB receptor exists as a heterodimer of two components, subunits GABAB(1) and GABAB(2).
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