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

被引：61

作者：

Wichmann, J ^{[1
]}

Adam, G ^{[1
]}

Röver, S ^{[1
]}

Cesura, AM ^{[1
]}

Dautzenberg, FM ^{[1
]}

Jenck, F ^{[1
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Preclin CNS Res, Div Pharma, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(99)00385-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 orphanin FQ (OFQ) and opioid (mu, kappa, delta) receptors. The influence of stereochemistry as well as the substitution pattern of the phenyl-ring in position 1 on the affinity for the orphanin FQ receptor and selectivity to opioid (mu, kappa, delta) receptors is discussed. The most interesting compound Ic was tested for its anxiolytic-like properties in vivo. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2343 / 2348

页数：6

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