Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors.

In conclusion, the molecular origins of subtype-selectivity exhibited by benzodiazepine-site modulators seem more complex than previously appreciated, and the importance of the α1-Gly201/α3-Glu225 residue for both potency- and efficacy-based subtype-selective modulation through this site is likely to be rooted in different molecular mechanisms.
PMID: 30121248 [PubMed - as supplied by publisher]

Source: Biochemical Pharmacology - August 16, 2018 Category: Drugs & Pharmacology Authors: Cecilia Söderhielm P, Balle T, Bak-Nyhus S, Zhang M, Hansen KM, Ahring PK, Jensen AA Tags: Biochem Pharmacol Source Type: research