Synthesis and Receptor Binding Studies of α5 GABA_AR Selective Novel Imidazodiazepines Targeted for Psychiatric and Cognitive Disorders.

ABSTRACT: GABA mediates inhibitory actions through various GABA_A receptor subtypes, including 19 subunits in human GABAAR. Dysregulation of GABAergic neurotransmission is associated with several psychiatric disorders, including depression, anxiety, and schizophrenia. Selective targeting of α2/3 GABAARs can treat mood and anxiety, while α5 GABAA-Rs can treat anxiety, depression, and cognitive performance. GL-II-73 and MP-III-022, α5-positive allosteric modulators have shown promising results in animal models of chronic stress, aging, and cognitive disorders, including MDD, schizophrenia, autism, and Alzheimer's disease. Described in this article is how small changes in the structure of imidazodiazepine substituents can greatly impact the subtype selectivity of benzodiazepine GABAAR. To inv

SUBMITTER: Sharmin D 

PROVIDER: S-EPMC10303271 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature