GABA-based therapeutic approaches: GABAA receptor subtype functions.

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97

作者:

U RudolphH M?Hler

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摘要:

It is increasingly being appreciated that GABA A receptor subtypes, through their specific regional, cellular and subcellular localization, are linked to distinct neuronal circuits and consequently serve distinct functions. GABA A receptor subtype-selective drugs are therefore expected to provide novel pharmacological profiles. Receptors containing the α 1 subunit mediate sedation and serve as targets for sedative hypnotics. Agonists selective for α2- and/or α3-containing GABA A receptors have been shown to provide anxiolysis without sedation in preclinical models, whereas inverse agonists selective for α5-containing GABA A receptors provide memory enhancement. Agonists selective for α3-containing GABA A receptors might be suitable for the treatment of deficits in sensorimotor processing in psychiatric disorders. Thus, a new pharmacology based on GABA A receptor subtype-specific actions is emerging.

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DOI:

10.1016/j.coph.2005.10.003

被引量:

685

年份:

2006

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