Tricyclic antipsychotics and antidepressants can inhibit α5-containing GABA_A receptors by two distinct mechanisms.

ABSTRACT:

Background and purpose

Many psychotherapeutic drugs, including clozapine, display polypharmacology and act on GABA_A receptors. Patients with schizophrenia show alterations in function, structure and molecular composition of the hippocampus, and a recent study demonstrated aberrant levels of hippocampal α5 subunit-containing GABA_A receptors. The purpose of this study is to investigate the effects of tricyclic compounds on α5 subunit-containing receptor subtypes.

Experimental approach

Functional studies of effects by seven antipsychotic and antidepressant medications were performed in several GABA_A receptor subtypes by two-electrode voltage-clamp electrophysiology using Xenopus laevis oocytes. Computational structural analysis was employed to d

SUBMITTER: Bampali K 

PROVIDER: S-EPMC9314015 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature