Discovery of a highly potent, functionally-selective muscarinic M-1 agonist,WAY-132983 using rational drug design and receptor modelling

Authors
Sabb, AL Husbands, GM Tokolics, J Stein, RP Tasse, RP Boast, CA Moyer, JA Abou-Gharbia, M
Citation
Al. Sabb et al., Discovery of a highly potent, functionally-selective muscarinic M-1 agonist,WAY-132983 using rational drug design and receptor modelling, BIOORG MED, 9(14), 1999, pp. 1895-1900
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
14
Year of publication
1999
Pages
1895 - 1900
Database
ISI
SICI code
0960-894X(19990719)9:14<1895:DOAHPF>2.0.ZU;2-X
Abstract
Rational drug design utilizing a receptor homology model of the human musca rinic M-1 receptor led to the discovery of the highly potent (K-i = 2 nM), efficacious, and in vivo functionally-selective M-1 agonist, WAY-132983. (C ) 1999 Elsevier Science Ltd. All rights reserved.