Discovery of a Biased Allosteric Modulator for Cannabinoid 1 Receptor: Preclinical Anti-Glaucoma Efficacy.
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DOI: 10.1021/acs.jmedchem.1c00040
Abstract: We apply the magic methyl effect to improve the potency/efficacy of GAT211, the prototypic 2-phenylindole-based cannabinoid type-1 receptor (CB1R) agonist-positive allosteric modulator (ago-PAM). Introducing a methyl group at the α-position of nitro group generated two… read more here.
Keywords: allosteric modulator; cb1r allosteric; efficacy; glaucoma ... See more keywords