N-[1-(2-phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists

Authors
Fujio, M Kuroita, T Sakai, Y Nakagawa, H Matsumoto, Y
Citation
M. Fujio et al., N-[1-(2-phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists, BIOORG MED, 10(21), 2000, pp. 2457-2461
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
21
Year of publication
2000
Pages
2457 - 2461
Database
ISI
SICI code
0960-894X(20001106)10:21<2457:NAN5>2.0.ZU;2-J
Abstract
A series of 1-adamantanecarboxamides was synthesized and examined for their potency as a selective 5-HT2 receptor antagonist. We found (S)-N-{1 -[2-(4 -fluorophenyl)ethyl]pyrrolidin-3-yl}-1-adamantanecarboxamide hydrochloride hydrate (10-(S), Y-39241) to have a high affinity and selectivity for 5-HT2 receptors, and this potent anti-platelet effect of Y-39241 was confirmed b oth in vitro and in vivo. (C) 2000 Elsevier Science Ltd. All rights reserve d.