GABA Receptors and the Pharmacology of Sleep.

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Title: GABA Receptors and the Pharmacology of Sleep.
Authors: Wisden, W
Yu, X
Franks, NP
Item Type: Journal Article
Abstract: Current GABAergic sleep-promoting medications were developed pragmatically, without making use of the immense diversity of GABAA receptors. Pharmacogenetic experiments are leading to an understanding of the circuit mechanisms in the hypothalamus by which zolpidem and similar compounds induce sleep at α2βγ2-type GABAA receptors. Drugs acting at more selective receptor types, for example, at receptors containing the α2 and/or α3 subunits expressed in hypothalamic and brain stem areas, could in principle be useful as hypnotics/anxiolytics. A highly promising sleep-promoting drug, gaboxadol, which activates αβδ-type receptors failed in clinical trials. Thus, for the time being, drugs such as zolpidem, which work as positive allosteric modulators at GABAA receptors, continue to be some of the most effective compounds to treat primary insomnia.
Issue Date: 10-Oct-2017
Date of Acceptance: 11-Sep-2017
URI: http://hdl.handle.net/10044/1/55730
DOI: https://dx.doi.org/10.1007/164_2017_56
ISSN: 0171-2004
Journal / Book Title: Handb Exp Pharmacol
Copyright Statement: © Springer International Publishing AG 2017. The final publication is available at Springer via https://link.springer.com/chapter/10.1007%2F164_2017_56
Sponsor/Funder: Wellcome Trust
Wellcome Trust
Wellcome Trust
Wellcome Trust
Wellcome Trust
Funder's Grant Number: 057279/Z/99/Z
057279/Z/99/Z
107839/Z/15/Z
107841/Z/15/Z
107841/Z/15/Z
Keywords: Benzodiazepine
GABA-A receptor
GABA-B receptor
Gaboxadol
Histamine
Sedation
Steroid
THIP
Z-drug
Zolpidem
Publication Status: Published online
Conference Place: Germany
Appears in Collections:Faculty of Natural Sciences



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