Different Benzodiazepines Bind with Distinct Binding Modes to GABA_A Receptors.

ABSTRACT: Benzodiazepines are clinically relevant drugs that bind to GABA_A neurotransmitter receptors at the α+/γ2- interfaces and thereby enhance GABA-induced chloride ion flux leading to neuronal hyperpolarization. However, the structural basis of benzodiazepine interactions with their high-affinity site at GABA_A receptors is controversially debated in the literature, and in silico studies led to discrepant binding mode hypotheses. In this study, computational docking of diazepam into α+/γ2- homology models suggested that a chiral methyl group, which is known to promote preferred binding to α5-containing GABA_A receptors (position 3 of the seven-membered diazepine ring), could possibly provide experimental evidence that supports or contradicts the proposed binding m

SUBMITTER: Elgarf AA 

PROVIDER: S-EPMC6102643 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature