{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,4]],"date-time":"2026-10-04T09:14:28Z","timestamp":1791105268349,"version":"4.1.0"},"reference-count":36,"publisher":"Portland Press Ltd.","issue":"6","content-domain":{"domain":["portlandpress.com"],"crossmark-restriction":true},"short-container-title":[],"published-print":{"date-parts":[[2009,12,1]]},"abstract":"<jats:p>GABAARs [GABA (\u03b3-aminobutyric acid) type-A receptors] are heteropentameric chloride-selective ligand-gated ion channels that mediate fast inhibition in the brain and are key therapeutic targets for benzodiazepines, barbiturates, neurosteroids and general anaesthetics. In the brain, most of the benzodiazepine-sensitive synaptic receptor subtypes are assembled from \u03b11-3, \u03b21-3 and \u03b32 subunits. Although it is evident that the pharmacological manipulation of GABAAR function can have profound effects on behaviour, the endogenous mechanisms that neurons use to promote sustained changes in the efficacy of neuronal inhibition remain to be documented. It is increasingly clear that GABAARs undergo significant rates of constitutive endocytosis and regulate recycling processes that can determine the efficacy of synaptic inhibition. Their endocytosis is regulated via the direct binding of specific endocytosis motifs within the intracellular domains of receptor \u03b21-3and \u03b32 subunits to the clathrin adaptor protein AP2 (adaptor protein 2). These binding motifs contain major sites of both serine and tyrosine phosphorylation within GABAARs. Their phosphorylation can have dramatic effects on binding to AP2. In the present review, we evaluate the role that these phospho-dependent interactions play in regulating the construction of inhibitory synapses, efficacy of neuronal inhibition and neuronal structure.<\/jats:p>","DOI":"10.1042\/bst0371355","type":"journal-article","created":{"date-parts":[[2009,11,19]],"date-time":"2009-11-19T18:02:29Z","timestamp":1258653749000},"page":"1355-1358","update-policy":"https:\/\/doi.org\/10.1042\/crossmark_policy","source":"Crossref","is-referenced-by-count":39,"title":["The role of GABAAR phosphorylation in the construction of inhibitory synapses and the efficacy of neuronal inhibition"],"prefix":"10.1042","volume":"37","author":[{"given":"Mansi","family":"Vithlani","sequence":"first","affiliation":[{"name":"Department of Neuroscience, Tufts University, 136 Harrison Ave, Boston, MA 02111, U.S.A., and Department of Neuroscience, Physiology and Pharmacology, University College London, Gower Street, London WC1E 6BT, U.K."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Stephen\u00a0J.","family":"Moss","sequence":"additional","affiliation":[{"name":"Department of Neuroscience, Tufts University, 136 Harrison Ave, Boston, MA 02111, U.S.A., and Department of Neuroscience, Physiology and Pharmacology, University College London, Gower Street, London WC1E 6BT, U.K."}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"288","published-online":{"date-parts":[[2009,11,19]]},"reference":[{"key":"2021111719332965300_B1","doi-asserted-by":"crossref","first-page":"665","DOI":"10.1016\/0896-6273(89)90235-3","article-title":"The structure of ion channels in membranes of excitable cells","volume":"3","author":"Unwin","year":"1989","journal-title":"Neuron"},{"key":"2021111719332965300_B2","doi-asserted-by":"crossref","first-page":"795","DOI":"10.2174\/1568026023393507","article-title":"Subunit composition, distribution and function of GABAA receptor subtypes","volume":"2","author":"Sieghart","year":"2002","journal-title":"Curr. 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