The complexity of the GABAA receptor shapes unique pharmacological profiles

Gamma-amino butyric acid (GABA) is the most abundant inhibitory neurotransmitter in the central nervous system (CNS) and many physiological actions are modulated by GABA(A) receptors. These chloride channels can be opened by GABA and are a target for a variety of important drugs such as benzodiazepi...

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Bibliographic Details
Published in:Drug discovery today 2009-09, Vol.14 (17-18), p.866-875
Main Authors: D'HULST, Charlotte, ATACK, John R, KOOY, R. Frank
Format: Article
Language:English
Subjects:
Animals
Benzodiazepines - pharmacology
Binding Sites - drug effects
Biological and medical sciences
Brain - metabolism
Drug Delivery Systems
Drug Discovery
gamma-Aminobutyric Acid - metabolism
General pharmacology
Humans
Medical sciences
Mice
Mice, Transgenic
Models, Biological
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Receptors, GABA-A - chemistry
Receptors, GABA-A - drug effects
Receptors, GABA-A - genetics
Receptors, GABA-A - metabolism
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Summary:Gamma-amino butyric acid (GABA) is the most abundant inhibitory neurotransmitter in the central nervous system (CNS) and many physiological actions are modulated by GABA(A) receptors. These chloride channels can be opened by GABA and are a target for a variety of important drugs such as benzodiazepines, barbiturates, neuroactive steroids, convulsants and anaesthetics. GABA(A) receptors are involved in anxiety, feeding and drinking behaviour, circadian rhythm, cognition, vigilance, and learning and memory. Moreover, deficits in the functional expression of GABA(A) receptors have been implicated in multiple neurological and psychiatric diseases. This review aims to discuss the unique physiological and pharmacological properties of the multitude of GABA(A) receptor subtypes present in the CNS, making this receptor an important target for novel rational drug therapy.
ISSN:1359-6446
1878-5832
DOI:10.1016/j.drudis.2009.06.009