Limiting Activity at β1-Subunit-Containing GABAA Receptor Subtypes Reduces Ataxia
@article{Gee2010LimitingAA, title={Limiting Activity at $\beta$1-Subunit-Containing GABAA Receptor Subtypes Reduces Ataxia}, author={Kelvin W. Gee and Minhtam B. Tran and Derk J. Hogenkamp and Timothy B C Johnstone and Rudy E Bagnera and Ryan F. Yoshimura and Jin-Cheng Huang and James D. Belluzzi and Edward R. Whittemore}, journal={Journal of Pharmacology and Experimental Therapeutics}, year={2010}, volume={332}, pages={1040 - 1053} }
GABAA receptor (R) positive allosteric modulators that selectively modulate GABAARs containing β2- and/or β3- over β1-subunits have been reported across diverse chemotypes. Examples include loreclezole, mefenamic acid, tracazolate, and etifoxine. In general,“β2/3-selective” GABAAR positive allosteric modulators are nonbenzodiazepines (nonBZs), do not show α-subunit isoform selectivity, yet have anxiolytic efficacy with reduced ataxic/sedative effects in animal models and humans. Here, we report…
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