Trends Pharmacol Sci. 2001 Apr;22(4):188-94.

GABA(A) receptor subtypes: dissecting their pharmacological functions.

Source

Institute of Pharmacology and Toxicology,University of Zürich and Swiss Federal Institut of Technology (ETH) Zürich, Winterthurerstrasse 190, CH-8057, Zürich, Switzerland. rudolph@pharma.unizh.ch

Abstract

The enhancement of GABA-mediated synaptic transmission underlies the pharmacotherapy of various neurological and psychiatric disorders. GABA(A) receptors are pluripotent drug targets that display an extraordinary structural heterogeneity: they are assembled from a repertoire of at least 18 subunits (alpha1-6, beta1-3, gamma1-3, delta, epsilon, theta, rho1-3). However, differentiating defined GABA(A) receptor subtypes on the basis of function has had to await recent progress in the genetic dissection of receptor subtypes in vivo. Evidence that the various actions of allosteric modulators of GABA(A) receptors, in particular the benzodiazepines, can be attributed to specific GABA(A) receptor subtypes will be discussed. Such discoveries could open up new avenues for drug development.

Comment in

Trends Pharmacol Sci. 2001 Aug;22(8):402-3.

PMID:: 11282419; [PubMed - indexed for MEDLINE]

Publication Types, MeSH Terms, Substances

Publication Types

Review

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

Other Literature Sources

Labome Researcher Resource - ExactAntigen/Labome

Medical

Neurologic Diseases - MedlinePlus Health Information

Supplemental Content

Related citations

Review Analysis of GABAA receptor function and dissection of the pharmacology of benzodiazepines and general anesthetics through mouse genetics. [Annu Rev Pharmacol Toxicol. 2004]
Review Analysis of GABAA receptor function and dissection of the pharmacology of benzodiazepines and general anesthetics through mouse genetics.
Rudolph U, Möhler H. Annu Rev Pharmacol Toxicol. 2004; 44:475-98.
Review The value of genetic and pharmacological approaches to understanding the complexities of GABA(A) receptor subtype functions: the anxiolytic effects of benzodiazepines. [Pharmacol Biochem Behav. 2008]
Review The value of genetic and pharmacological approaches to understanding the complexities of GABA(A) receptor subtype functions: the anxiolytic effects of benzodiazepines.
Reynolds DS. Pharmacol Biochem Behav. 2008 Jul; 90(1):37-42. Epub 2008 Mar 28.
Altered receptor subtypes in the forebrain of GABA(A) receptor delta subunit-deficient mice: recruitment of gamma 2 subunits. [Neuroscience. 2002]
Altered receptor subtypes in the forebrain of GABA(A) receptor delta subunit-deficient mice: recruitment of gamma 2 subunits.
Korpi ER, Mihalek RM, Sinkkonen ST, Hauer B, Hevers W, Homanics GE, Sieghart W, Lüddens H. Neuroscience. 2002; 109(4):733-43.
Review The GABA-A receptor gene family: new targets for therapeutic intervention. [Neurochem Int. 1999]
Review The GABA-A receptor gene family: new targets for therapeutic intervention.
Whiting PJ. Neurochem Int. 1999 May; 34(5):387-90.
Review Validation of GABA(A) receptor subtypes as potential drug targets by using genetically modified mice. [Curr Drug Targets CNS Neurol Disord. 2003]
Review Validation of GABA(A) receptor subtypes as potential drug targets by using genetically modified mice.
Rosahl TW. Curr Drug Targets CNS Neurol Disord. 2003 Aug; 2(4):207-12.

See reviews... See all...

Cited by 38 PubMed Central articles

Clobazam as an adjunctive therapy in treating seizures associated with Lennox-Gastaut syndrome. [Neuropsychiatr Dis Treat. 2011]
Clobazam as an adjunctive therapy in treating seizures associated with Lennox-Gastaut syndrome.
Leahy JT, Chu-Shore CJ, Fisher JL. Neuropsychiatr Dis Treat. 2011; 7:673-81. Epub 2011 Nov 11.
Pathophysiological aspects of diversity in neuronal inhibition: a new benzodiazepine pharmacology. [Dialogues Clin Neurosci. 2002]
Pathophysiological aspects of diversity in neuronal inhibition: a new benzodiazepine pharmacology.
Möhler H. Dialogues Clin Neurosci. 2002 Sep; 4(3):261-9.
The biology of fear- and anxiety-related behaviors. [Dialogues Clin Neurosci. 2002]
The biology of fear- and anxiety-related behaviors.
Steimer T. Dialogues Clin Neurosci. 2002 Sep; 4(3):231-49.

See all...

Related information

Related Citations
Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
Compound (MeSH Keyword)
PubChem chemical compound records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Substance (MeSH Keyword)
PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Cited in PMC
Full-text articles in the PubMed Central Database that cite the current articles.
Cited in Books
NCBI Bookshelf books that cite the current articles.

Recent activity

Clear Turn Off Turn On

GABA(A) receptor subtypes: dissecting their pharmacological functions.
GABA(A) receptor subtypes: dissecting their pharmacological functions.
Trends Pharmacol Sci. 2001 Apr ;22(4):188-94.

PubMed
Genetic analysis of an overlapping functional requirement for L1- and NCAM-type ...
Genetic analysis of an overlapping functional requirement for L1- and NCAM-type proteins during sensory axon guidance in Drosophila.
Mol Cell Neurosci. 2005 Jan ;28(1):141-52.

PubMed
The life span determinant p66Shc localizes to mitochondria where it associates w...
The life span determinant p66Shc localizes to mitochondria where it associates with mitochondrial heat shock protein 70 and regulates trans-membrane potential.
J Biol Chem. 2004 Jun 11 ;279(24):25689-95. Epub 2004 Apr 12 .

PubMed
A conserved role for Drosophila Neuroglian and human L1-CAM in central-synapse f...
A conserved role for Drosophila Neuroglian and human L1-CAM in central-synapse formation.
Curr Biol. 2006 Jan 10 ;16(1):12-23.

PubMed
Effects of damping head movement and facial expression in dyadic conversation us...
Effects of damping head movement and facial expression in dyadic conversation using real-time facial expression tracking and synthesized avatars.
Philos Trans R Soc Lond B Biol Sci. 2009 Dec 12 ;364(1535):3485-95.

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Display Settings:

Send to: