8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivativesas orphanin FQ receptor agonists

Citation
J. Wichmann et al., 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivativesas orphanin FQ receptor agonists, BIOORG MED, 9(16), 1999, pp. 2343-2348
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
16
Year of publication
1999
Pages
2343 - 2348
Database
ISI
SICI code
0960-894X(19990816)9:16<2343:8D>2.0.ZU;2-W
Abstract
A series of 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives 1 was studied with respect to the binding affinity for the orph anin FQ (OFQ) and opioid (mu, kappa, delta) receptors. The influence of ste reochemistry as well as the substitution pattern of the phenyl-ring in posi tion 1 on the affinity for the orphanin FQ receptor and selectivity to opio id (mu, kappa, delta) receptors is discussed. The most interesting compound Ic was tested for its anxiolytic-like properties in vivo. (C) 1999 Elsevie r Science Ltd. All rights reserved.