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ID: ALA1132775
Journal: Bioorg Med Chem Lett
Title: N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.
Authors: Tsai Y, Dukat M, Slassi A, MacLean N, Demchyshyn L, Savage JE, Roth BL, Hufesein S, Lee M, Glennon RA.
Abstract: N-Benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine (BS/5-OMe DMT; 5) was shown to bind at human 5-HT6 serotonin receptors with high affinity (Ki = 2.3 nM) relative to serotonin (Ki = 78 nM). Structural variation failed to result in significantly enhanced affinity. BS/5-OMe DMT acts as an antagonist of 5-HT-stimulated adenylate cyclase (pA2 = 8.88 nM) and may represent the first member of a novel class of 5-HT6 antagonists.
CiteXplore: 11055342