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J Med Chem. 2003 Dec 4;46(25):5505-11.

Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.

Author information

1
Department of Pharmacy and Pharmacology, University of Bath, Bath, BA2 7AY, UK.

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.

PMID:
14640558
DOI:
10.1021/jm0309203
[Indexed for MEDLINE]

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