8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one Derivatives As Orphanin FQ Receptor Agonists

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 1999 Sep 7

PMID 10476866

Citations 23

Authors

J Wichmann

G Adam

S Rover

A M Cesura

F M Dautzenberg

F Jenck

Affiliations

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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 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 1c was tested for its anxiolytic-like properties in vivo.

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