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

doi:10.1021/jm0309203

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

Chemistry & Biochemistry

Research output: Contribution to journal › Article › peer-review

14 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 language	English (US)
Pages (from-to)	5505-5511
Number of pages	7
Journal	Journal of medicinal chemistry
Volume	46
Issue number	25
DOIs	https://doi.org/10.1021/jm0309203
State	Published - Dec 4 2003

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AU - Black, Shannon L.

AU - Chauvignac, Cedric

AU - Grundt, Peter

AU - Miller, Carl N.

AU - Wood, Susan

AU - Traynor, John R.

AU - Lewis, John W.

AU - Husbands, Stephen M.

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

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