GABA-based therapeutic approaches: GABAA receptor subtype functions

Uwe Rudolph, Hanns Möhler

Research output: Contribution to journalReview articlepeer-review

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 α1 subunit mediate sedation and serve as targets for sedative hypnotics. Agonists selective for α2- and/or α3-containing GABAA receptors have been shown to provide anxiolysis without sedation in preclinical models, whereas inverse agonists selective for α5-containing GABAA receptors provide memory enhancement. Agonists selective for α3-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.

Original languageEnglish (US)
Pages (from-to)18-23
Number of pages6
JournalCurrent Opinion in Pharmacology
Volume6
Issue number1 SPEC. ISS.
DOIs
StatePublished - Feb 2006
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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