2010PubMedRequires access

[GABA B-type receptors: structure and functions].

В. Н. Перфилова, Tiurenkov In

Open publisher page 2 citations

Abstract

Available data on structure, localization, physiology and pharmacology of GABAB-type receptors are reviewed. GABAB-receptors are pre- and postsynaptically located, belong to metabotropic ones and are connected to trimeric G-protein. Mammal GABAB-receptors, consisting of two subunits of B1 and B2 type, are allosterically regulated heterodimers (actively functioning GABAB-receptors). The activation of GABAB-type receptors leads to increasing K+ release from the cell and hyperpolarization of cell membrane. GABAB-receptors are also connected with potentially dependent Ca2+ channels, which are involved in the synaptic release of neurotransmitters. There is a great number of their allosteric modulators, agonists and antagonists.

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What this paper is about

Available data on structure, localization, physiology and pharmacology of GABAB-type receptors are reviewed. GABAB-receptors are pre- and postsynaptically located, belong to metabotropic ones and are connected to trimeric G-protein. Mammal GABAB-receptors, consisting of two subunits of B1 and B2 type, are allosterically regulated heterodimers (actively functioning GABAB-receptors). The activation of GABAB-type receptors leads to increasing K+ release from the cell and hyperpolarization of cell membrane. GABAB-receptors are also connected with potentially dependent Ca2+ channels, which are involved in the synaptic release of neurotransmitters. There is a great number of their allosteric modulators, agonists and antagonists.

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Available abstract

Available data on structure, localization, physiology and pharmacology of GABAB-type receptors are reviewed. GABAB-receptors are pre- and postsynaptically located, belong to metabotropic ones and are connected to trimeric G-protein. Mammal GABAB-receptors, consisting of two subunits of B1 and B2 type, are allosterically regulated heterodimers (actively functioning GABAB-receptors). The activation of GABAB-type receptors leads to increasing K+ release from the cell and hyperpolarization of cell membrane. GABAB-receptors are also connected with potentially dependent Ca2+ channels, which are involved in the synaptic release of neurotransmitters. There is a great number of their allosteric modulators, agonists and antagonists.

Key concepts: GABAB receptor, Metabotropic receptor, Class C GPCR, Receptor, Allosteric regulation, Rhodopsin-like receptors, Chemistry, GABAA receptor

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