| Literature DB >> 14640558 |
Shannon L Black1, Cedric Chauvignac, Peter Grundt, Carl N Miller, Susan Wood, John R Traynor, John W Lewis, Stephen M Husbands.
Abstract
Derivatives of the highly selective kappa-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 kappa-affinity and antagonist potency. Disubstitution of the guanidino moiety led to reduced kappa-selectivity.Entities:
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Year: 2003 PMID： 14640558 DOI： 10.1021/jm0309203
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446