GABA-based therapeutic approaches: GABAA receptor subtype functions.

Abstract:

:It is increasingly being appreciated that GABAA receptor subtypes, through their specific regional, cellular and subcellular localization, are linked to distinct neuronal circuits and consequently serve distinct functions. GABAA receptor subtype-selective drugs are therefore expected to provide novel pharmacological profiles. Receptors containing the alpha1 subunit mediate sedation and serve as targets for sedative hypnotics. Agonists selective for alpha2- and/or alpha3-containing GABAA receptors have been shown to provide anxiolysis without sedation in preclinical models, whereas inverse agonists selective for alpha5-containing GABAA receptors provide memory enhancement. Agonists selective for alpha3-containing GABAA receptors might be suitable for the treatment of deficits in sensorimotor processing in psychiatric disorders. Thus, a new pharmacology based on GABAA receptor subtype-specific actions is emerging.

journal_name

Curr Opin Pharmacol

authors

Rudolph U,Möhler H

doi

10.1016/j.coph.2005.10.003

keywords:

subject

Has Abstract

pub_date

2006-02-01 00:00:00

pages

18-23

issue

1

eissn

1471-4892

issn

1471-4973

pii

S1471-4892(05)00186-4

journal_volume

6

pub_type

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