THE SEROTONIN 5-HT4 RECEPTOR .3. DESIGN AND PHARMACOLOGICAL EVALUATION OF A NEW CLASS OF ANTAGONISTS

Authors
BUCHHEIT KH KLEIN F KLOPPNER E PFANNKUCHE HJ MATTES H
Citation
Kh. Buchheit et al., THE SEROTONIN 5-HT4 RECEPTOR .3. DESIGN AND PHARMACOLOGICAL EVALUATION OF A NEW CLASS OF ANTAGONISTS, Bioorganic & medicinal chemistry letters, 5(21), 1995, pp. 2495-2500
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
21
Year of publication
1995
Pages
2495 - 2500
Database
ISI
SICI code
0960-894X(1995)5:21<2495:TS5R.D>2.0.ZU;2-B
Abstract
The design, synthesis and pharmacological activity of a new class of p otent and selective 5-HT4 receptor antagonists containing an indole nu cleus linked to a carbazimidamide are presented. 4c, a representative member of our new class is a potent competitive antagonist at 5-HT4 re ceptors with a pA(2) value of 8.4, displaying selectivity (ranging fro m 20 to over 1000 fold) versus other serotonin receptor subtypes.