5-alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists

Authors
Slassi, A Edwards, L O'Brien, A Meng, CQ Xin, T Seto, C Lee, DKH MacLean, N Hynd, D Chen, C Wang, H Kamboj, R Rakhit, S
Citation
A. Slassi et al., 5-alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists, BIOORG MED, 10(15), 2000, pp. 1707-1709
Citations number
26
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
15
Year of publication
2000
Pages
1707 - 1709
Database
ISI
SICI code
0960-894X(20000807)10:15<1707:5DAHSA>2.0.ZU;2-2
Abstract
A series of 5-alkyltryptamines (6) and the corresponding conformationally c onstrained analogues (8) have been synthesized. The structure-activity rela tionships (SAR) at the 5-position of the indole skeleton and the ethylamine side chain have been studied. Functional activities were assessed using is olated rabbit saphenous vein. Potent, selective ligands were found (6e, K-i 2.5 nM, 5-HT1B/5-HT1D 125-fold) that have potential for treating acute mig raine. (C) 2000 Elsevier Science Ltd. All rights reserved.