Guanidino N-Substituted and N,N-Disubstituted Derivatives of the κ-Opioid Antagonist GNTI

Shannon L. Black, Cedric Chauvignac, Peter Grundt, Carl N. Miller, Susan Wood, John R. Traynor, John W. Lewis, Stephen M. Husbands

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

Derivatives of the highly selective κ-opioid receptor antagonist GNTI (2a) have been prepared. Binding and functional studies conducted on cloned human opioid receptors expressed in Chinese hamster ovarian (CHO) cells suggested that adding a benzyl or a substituted benzyl group to the guanidino moiety led, in general, to a retention of high κ-affinity and antagonist potency. Disubstitution of the guanidino moiety led to reduced κ-selectivity.

Original languageEnglish (US)
Pages (from-to)5505-5511
Number of pages7
JournalJournal of medicinal chemistry
Volume46
Issue number25
DOIs
StatePublished - Dec 4 2003

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