Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists

Authors
Boyd, RE Carson, JR Codd, EE Gauthier, AD Neilson, LA Zhang, SP
Citation
Re. Boyd et al., Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists, BIOORG MED, 10(10), 2000, pp. 1109-1111
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
10
Year of publication
2000
Pages
1109 - 1111
Database
ISI
SICI code
0960-894X(20000515)10:10<1109:SABAO4>2.0.ZU;2-Q
Abstract
A series of 4-diarylaminotropanes has been prepared. Both endo and exo dias tereomeric forms bound to the delta opioid receptor but the endo isomers we re more potent and selective versus the mu opioid receptor than the exo iso mers. The most potent delta opioid agonist (14) exhibited a delta opioid K- i of 0.2 nM and was 860-fold selective over mu. (C) 2000 Elsevier Science L td. All rights reserved.