Benzodiazepine Modulation of GABA_A Receptors: A Mechanistic Perspective.

ABSTRACT: Benzodiazepines (BZDs) are a class of widely prescribed psychotropic drugs that target GABA_A receptors (GABA_ARs) to tune inhibitory synaptic signaling throughout the central nervous system. Despite knowing their molecular target for over 40 years, we still do not fully understand the mechanism of modulation at the level of the channel protein. Nonetheless, functional studies, together with recent cryo-EM structures of GABA_A(α1)₂(βX)₂(γ2)₁ receptors in complex with BZDs, provide a wealth of information to aid in addressing this gap in knowledge. Here, mechanistic interpretations of functional and structural evidence for the action of BZDs at GABA_A(α1)₂(βX)₂(γ2)₁ receptors are review

SUBMITTER: Goldschen-Ohm MP 

PROVIDER: S-EPMC9775625 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature