TY - JOUR
T1 - GABA-based therapeutic approaches
T2 - GABAA receptor subtype functions
AU - Rudolph, Uwe
AU - Möhler, Hanns
N1 - Funding Information:
Work in the authors’ laboratories was funded by the Swiss National Science Foundation.
PY - 2006/2
Y1 - 2006/2
N2 - 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.
AB - 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.
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U2 - 10.1016/j.coph.2005.10.003
DO - 10.1016/j.coph.2005.10.003
M3 - Review article
C2 - 16376150
AN - SCOPUS:30844456191
SN - 1471-4892
VL - 6
SP - 18
EP - 23
JO - Current Opinion in Pharmacology
JF - Current Opinion in Pharmacology
IS - 1 SPEC. ISS.
ER -