2-METHOXY-N-(1-AZABICYCLO[2.2.2]OCT-3-YL)BENZAMIDE (TRIZAC), A HIGH-AFFINITY LIGAND FOR THE 5-HT-3 RECEPTOR

Authors
DEPAULIS T TRIVEDI BL ZHANG ZJ SCHMIDT DE EBERT MH HEWLETT WA
Citation
T. Depaulis et al., 2-METHOXY-N-(1-AZABICYCLO[2.2.2]OCT-3-YL)BENZAMIDE (TRIZAC), A HIGH-AFFINITY LIGAND FOR THE 5-HT-3 RECEPTOR, Bioorganic & medicinal chemistry letters, 6(22), 1996, pp. 2657-2662
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
22
Year of publication
1996
Pages
2657 - 2662
Database
ISI
SICI code
0960-894X(1996)6:22<2657:2(AH>2.0.ZU;2-6
Abstract
TRIZAC is one of the most potent 5-HT-3 receptor antagonist reported t o date, having 20-fold higher affinity than (S)-5-iodozacopride. This high affinity (K-i 0.05 +/- 0.01 nM) and a moderate apparent Lipophili city (log P-app 2.12) makes TRIZAC a promising ligand for studying 5-H T-3 receptors. Copyright (C) 1996 Elsevier Science Ltd