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Reducing GABA Receptors

A number of important drugs act on GABA A receptors, pentameric GABA-gated chloride channels assembled from among 19 known subunits. In trying to discover the roles in the brain of the subunits and their combinations, with the goal of developing more selective drugs, one tool has been to reduce expr...

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Published in:Life Sciences 2003-08, Vol.73 (14), p.1741-1758
Main Author: Burt, David R
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Language:English
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description A number of important drugs act on GABA A receptors, pentameric GABA-gated chloride channels assembled from among 19 known subunits. In trying to discover the roles in the brain of the subunits and their combinations, with the goal of developing more selective drugs, one tool has been to reduce expression of the subunits and examine the functional consequences. After briefly examining the properties of GABA A receptors, this review surveys the means available for receptor subunit reduction, and some of the observations to which their application has led. The methods discussed include radiation-induced deletion, gene knockout, knock-in mutations, antisense, ribozymes, RNA interference, dominant negative constructs, and transcriptional regulation, e.g., via decoy oligonucleotides.
doi_str_mv 10.1016/S0024-3205(03)00505-8
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subjects Animals
Anxiolytic
Benzodiazepine
Brain - metabolism
Brain - physiology
Chromosome Deletion
Drug development
Gamma-aminobutyric acid
Humans
Knockdown
Oligonucleotides, Antisense - pharmacology
Protein Subunits
Receptors, GABA - biosynthesis
Receptors, GABA - genetics
Receptors, GABA - metabolism
Receptors, GABA - physiology
Receptors, GABA-A - biosynthesis
Receptors, GABA-A - genetics
Receptors, GABA-A - metabolism
Receptors, GABA-A - physiology
RNA Interference
Sedative
Silencing
title Reducing GABA Receptors
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