Activation of the Rat α1β2ε GABA_A Receptor by Orthosteric and Allosteric Agonists.

ABSTRACT: GABA_A receptors are a major contributor to fast inhibitory neurotransmission in the brain. The receptors are activated upon binding the transmitter GABA or allosteric agonists including a number of GABAergic anesthetics and neurosteroids. Functional receptors can be formed by various combinations of the nineteen GABA_A subunits cloned to date. GABA_A receptors containing the ε subunit exhibit a significant degree of constitutive activity and have been suggested to be unresponsive to allosteric agents. In this study, we have characterized the functional properties of the rat α1β2ε GABA_A receptor. We confirm that the α1β2ε receptor exhibits a higher level of constitutive activity than typical of GABA_A receptors and show that it is ineffica

SUBMITTER: Germann AL 

PROVIDER: S-EPMC9312946 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature