Limiting Activity at β1-Subunit-Containing GABAA Receptor Subtypes Reduces Ataxia

Limiting activity at beta1-subunit-containing GABAA receptor subtypes reduces ataxia.

GABA(A) receptor (R) positive allosteric modulators that selectively modulate GABA(A)Rs containing beta(2)- and/or beta(3)- over beta(1)-subunits have been reported across diverse chemotypes. Examples include loreclezole, mefenamic acid, tracazolate, and etifoxine. In general,"beta(2/3)-selective" GABA(A)R positive allosteric modulators are nonbenzodiazepines (nonBZs), do not show alpha-subunit...

Limiting Activity at 1-Subunit-Containing GABAA Receptor Subtypes Reduces Ataxia

GABAA receptor (R) positive allosteric modulators that selectively modulate GABAARs containing 2and/or 3over 1subunits have been reported across diverse chemotypes. Examples include loreclezole, mefenamic acid, tracazolate, and etifoxine. In general,“ 2/3-selective” GABAAR positive allosteric modulators are nonbenzodiazepines (nonBZs), do not show -subunit isoform selectivity, yet have anxiolyt...

GABAA receptor subunit gamma2 and delta subtypes confer unique kinetic properties on recombinant GABAA receptor currents in mouse fibroblasts.

1. To determine their contributions to the rapid kinetic properties of GABAA receptor (GABAR) currents, alpha1 and beta3 subunit subtypes without or with delta or gamma2L subtypes were transiently coexpressed in mouse L929 fibroblasts to produce alpha1beta3, alpha1beta3delta, or alpha1beta3gamma2L GABAR isoforms. 2. Brief (2-3 ms) applications of 1 mM GABA to outside-out membrane patches contai...

Alpha 2 subunit-containing GABAA receptor subtypes are up-regulated and contribute to alcohol-induced functional plasticity in rat hippocampus

α2 Subunit-Containing GABAA Receptor Subtypes Are Upregulated and Contribute to Alcohol-Induced Functional Plasticity in the Rat Hippocampus.

Alcohol (EtOH) intoxication causes changes in the rodent brain γ-aminobutyric acid receptor (GABAAR) subunit composition and function, playing a crucial role in EtOH withdrawal symptoms and dependence. Building evidence indicates that withdrawal from acute EtOH and chronic intermittent EtOH (CIE) results in decreased EtOH-enhanced GABAAR δ subunit-containing extrasynaptic and EtOH-insensitive α...