TY - JOUR
T1 - Beyond classical benzodiazepines
T2 - Novel therapeutic potential of GABA A receptor subtypes
AU - Rudolph, Uwe
AU - Knoflach, Frédéric
N1 - Funding Information:
Research by U.R. is supported by the National Institutes of Health (award numbers GM086448, MH080006, MH085149, DA027051, DA026578 and MH087829). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institute of General Medical Sciences, the National Institute of Mental Health and the National Institute on Drug Abuse, or the National Institutes of Health. The authors gratefully thank T. Ballard-Yardy, R. Gasser, M.-C. Hernandez, A. W. Thomas and G. Trube (all at Roche Basel) for discussions, ideas and support.
PY - 2011/9
Y1 - 2011/9
N2 - GABAA (γ-aminobutyric acid, type A) receptors are a family of ligand-gated ion channels that are essential for the regulation of central nervous system function. Benzodiazepines-which non-selectively target GABA A receptors containing the α1, α2, α3 or α5 subunits have been in clinical use for decades and are still among the most widely prescribed drugs for the treatment of insomnia and anxiety disorders. However, their use is limited by side effects and the risk of drug dependence. In the past decade, the identification of separable key functions of GABA A receptor subtypes suggests that receptor subtype-selective compounds could overcome the limitations of classical benzodiazepines; furthermore, they might be valuable for novel indications such as chronic pain, depression, schizophrenia, cognitive enhancement and stroke.
AB - GABAA (γ-aminobutyric acid, type A) receptors are a family of ligand-gated ion channels that are essential for the regulation of central nervous system function. Benzodiazepines-which non-selectively target GABA A receptors containing the α1, α2, α3 or α5 subunits have been in clinical use for decades and are still among the most widely prescribed drugs for the treatment of insomnia and anxiety disorders. However, their use is limited by side effects and the risk of drug dependence. In the past decade, the identification of separable key functions of GABA A receptor subtypes suggests that receptor subtype-selective compounds could overcome the limitations of classical benzodiazepines; furthermore, they might be valuable for novel indications such as chronic pain, depression, schizophrenia, cognitive enhancement and stroke.
UR - http://www.scopus.com/inward/record.url?scp=80052274158&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=80052274158&partnerID=8YFLogxK
U2 - 10.1038/nrd3502
DO - 10.1038/nrd3502
M3 - Review article
C2 - 21799515
AN - SCOPUS:80052274158
SN - 1474-1776
VL - 10
SP - 685
EP - 697
JO - Nature Reviews Drug Discovery
JF - Nature Reviews Drug Discovery
IS - 9
ER -