Article
Superagonist, Full Agonist, Partial Agonist, and Antagonist Actions of Arylguanidines at 5-Hydroxytryptamine-3 (5-HT3) Subunit A Receptors.
ACS chemical neuroscience - 16 Nov 2016
Alix Katie, Khatri Shailesh, Mosier Philip D, Casterlow Samantha, Yan Dong, Nyce Heather L, White Michael M, Schulte Marvin K, Dukat Małgorzata
Abstract excerpt
Introduction of minor variations to the substitution pattern of arylguanidine 5-hydroxytryptamine-3 (5-HT3) receptor ligands resulted in a broad spectrum of functionally-active ligands from antagonist to superagonist. For example, (i) introduction of an additional Cl-substituent(s) to our lead full agonist N-(3-chlorophenyl)guanidine (mCPG, 2; efficacy % = 106) yielded superagonists 7-9 (efficacy % = 186, 139,...
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