Pharmacological evaluation of enantiomerically separated positive allosteric modulators of cannabinoid 1 receptor, GAT591 and GAT593

Positive allosteric modulation of the type 1 cannabinoid receptor (CB1R) has substantial potential to treat both neurological and immune disorders. To date, a few studies have evaluated the structure-activity relationship (SAR) for CB1R positive allosteric modulators (PAMs). In this study, we separa...

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Bibliographic Details

Published in:	Frontiers in Pharmacology
Main Authors:	Asher L. Brandt, Sumanta Garai, Ayat Zagzoog, Dow P. Hurst, Lesley A. Stevenson, Roger G. Pertwee, Gregory H. Imler, Patricia H. Reggio, Ganesh A. Thakur, Robert B. Laprairie
Format:	Article
Language:	English
Published:	Frontiers Media S.A. 2022-10-01
Subjects:	type 1 cannabinoid receptor (CB1R) positive allosteric modulator allosteric agonist molecular pharmacology In silico modeling molecular mechanics-generalized born surface area (MMGBSA)
Online Access:	https://www.frontiersin.org/articles/10.3389/fphar.2022.919605/full