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.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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CHO Cells
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Cricetinae
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Guanidines / chemical synthesis*
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Guanidines / chemistry
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Guanidines / pharmacology
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Humans
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Morphinans / chemical synthesis*
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Morphinans / chemistry
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Morphinans / pharmacology
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Receptors, Opioid, kappa / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan
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Guanidines
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Morphinans
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Receptors, Opioid, kappa