N-1-(benzenesulfonyl)tryptamines as novel 5-HT6 antagonists

Authors
Tsai, YC Dukat, M Slassi, A MacLean, N Demchyshyn, L Savage, JE Roth, BL Hufesein, S Lee, M Glennon, RA
Citation
Yc. Tsai et al., N-1-(benzenesulfonyl)tryptamines as novel 5-HT6 antagonists, BIOORG MED, 10(20), 2000, pp. 2295-2299
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
20
Year of publication
2000
Pages
2295 - 2299
Database
ISI
SICI code
0960-894X(20001016)10:20<2295:NAN5A>2.0.ZU;2-S
Abstract
N-1-Benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine (BS/5-OMe DMT; 5) was shown to bind at human 5-HT6 serotonin receptors with high affinity (K-i = 2.3 nM) relative to serotonin (K-i = 78 nM). Structural variation failed to result in significantly enhanced affinity. BS/5-OMe DMT acts as an antagon ist of 5-HT-stimulated adenylate cyclase (pA(2) = 8.88 nM) and may represen t the first member of a novel class of 5-HT6 antagonists. (C) 2000 Elsevier Science Ltd. All rights reserved.