Definition
Anxiolytic and hypnotic drugs are used in the treatment of anxiety disorders and sleep disturbances to reduce anxiety and promote sleep. These drugs encompass a number of different classes of compounds, including the benzodiazepines. Most of the currently used anxiolytic and hypnotic drugs act on Ionotropic receptors for GABA, the major inhibitory neurotransmitter in the brain. This reflects the importance of GABAergic systems for anxiety and sleep related behaviours [1].
The focus of this essay is on compounds acting at ionotropic GABA receptors and the development of new anxiolytic and hypnotic drugs. There is great diversity in these receptors and of particular interest are compounds that show selectivity for specific subtypes of ionotropic GABA receptors.
Characteristics
Ionotropic GABA Receptors
Ionotropic GABA receptors comprise the GABAA and GABAC receptors, whereas GABAB receptors are metabotropic [2]. Ionotropic GABA receptors are ligand-gated ion channelsthat are...
This is a preview of subscription content, log in via an institution.
References
Möhler H (2006) GABAA receptors in central nervous system disease: anxiety, epilepsy, and insomnia. J Recept Signal Transduct 26:731–740
Johnston GAR (2005) GABAA receptor channel pharmacology. Current Pharm Des 11:159–164
Chebib M, Hanrahan JR, Mewett KN, Duke RK, Johnston GAR (2004) Ionotropic GABA receptors as therapeutic targets for memory and sleep disorders. Annu Rep Med Chem 39:13–23
Rudolph U, Möhler H (2004) Analysis of GABAA receptor function and dissection of the pharmacology of benzodiazepines and general anaesthetics through mouse genetics. Annu Rev Pharmacol Toxicol 44:475–498
Dawson GR, Collinson N, Atack JR (2007) Development of subtype selective GABAA modulators. CNS Spect 10:21–27
Gottesmann C (2002) GABA mechanisms and sleep. Neuroscience 111:231–239
Ebert B, Wafford KA, Deacon S (2006) Treating insomnia: current and investigational pharmacological approaches. Pharmacol Ther 112:612–629
Belelli D, Peden DR, Rosahl TW, Wafford KA, Lambert JJ (2005) Extrasynaptic GABAA receptors of thalamocortical neurons: a molecular target for hypnotics. J Neurosci 25:11513–11520
Lancel M, Wetter TC, Steiger A, Mathias S (2001) Effect of the GABAA agonist gaboxadol on nocturnal sleep and hormone secretion in healthy elderly subjects. Am J Physiol Endocrinol Metab 281:E130–E137
Johnston GAR, Hanrahan JR, Chebib M, Duke RK, Mewett KN (2006) Modulation of ionotropic GABA receptors by natural products of plant origin. Adv Pharmacol 54:285–316
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2008 Springer-Verlag GmbH Berlin Heidelberg
About this entry
Cite this entry
Hinton, T., Johnston, G.A.R. (2008). Anxiolytic and Hypnotic Drugs Acting on Ionotropic GABA Receptors. In: Binder, M.D., Hirokawa, N., Windhorst, U. (eds) Encyclopedia of Neuroscience. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-29678-2_306
Download citation
DOI: https://doi.org/10.1007/978-3-540-29678-2_306
Published:
Publisher Name: Springer, Berlin, Heidelberg
Print ISBN: 978-3-540-23735-8
Online ISBN: 978-3-540-29678-2
eBook Packages: Biomedical and Life SciencesReference Module Biomedical and Life Sciences