Molecular diversity, trafficking and subcellular localization of GABAB receptors.

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摘要：

GABA B receptors are the G-protein coupled receptors for the main inhibitory neurotransmitter in the brain, γ-aminobutyric acid (GABA). While native studies predicted pharmacologically distinct GABA B receptor subtypes, molecular studies failed to identify the expected receptor varieties. Mouse genetic experiments therefore addressed whether the cloned receptors can account for the classical electrophysiological, biochemical and behavioral GABA B responses or whether additional receptors exist. Among G-protein coupled receptors, GABA B receptors are unique in that they require 2 distinct subunits for functioning. This atypical receptor structure triggered a large body of work that investigated the regulation of receptor assembly and trafficking. With the availability of molecular tools, substantial progress was also made in the analysis of the receptor protein distribution in neuronal compartments. Here, we review recent studies that shed light on the molecular diversity, the subcellular distribution and the cell surface dynamics of GABA B receptors.

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关键词：

GABA B Compartmentalization Endocytosis Desensitization Tolerance

DOI：

10.1016/j.pharmthera.2006.03.006

被引量：

272

年份：

2006