2-aryl tryptamines: Selective high-affinity antagonists for the h5-HT2A receptor

Authors
Stevenson, GI Smith, AL Lewis, S Michie, SG Neduvelil, JG Patel, S Marwood, R Patel, S Castro, JL
Citation
Gi. Stevenson et al., 2-aryl tryptamines: Selective high-affinity antagonists for the h5-HT2A receptor, BIOORG MED, 10(24), 2000, pp. 2697-2699
Citations number
8
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
24
Year of publication
2000
Pages
2697 - 2699
Database
ISI
SICI code
0960-894X(200012)10:24<2697:2TSHAF>2.0.ZU;2-R
Abstract
A series of 2-aryl tryptamines have been identified as high-affinity h6-HT2 A antagonists. Structure-activity relationship studies have shown that h5-H T2A affinity can be attained via modifications to the tryptamine side chain and that selectivity over h5-HT2C and hD(2) receptors can be controlled by suitable C-2 aryl groups. (C) 2000 Elsevier Science Ltd. All rights reserv ed.