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pubmed-article:15743210pubmed:abstractTextIndolic N-benzylation of naltrindole reportedly extends the duration of delta-opioid receptor (DOR) antagonism. Similar modification of the kappa-opioid receptor (KOR) antagonist norBNI (1a) and its 17,17'-diNMe analogue (1d), a low potency mu-opioid receptor (MOR) partial agonist, was found to affect predominantly their MOR activity. When administered systemically in mouse antinociceptive assays, N-benzyl-norBNI (1b) had only MOR agonist activity of relatively short duration whereas on central administration it had only a KOR-antagonist action of extremely long duration.lld:pubmed
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pubmed-article:15743210pubmed:articleTitleMajor effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.lld:pubmed
pubmed-article:15743210pubmed:affiliationDepartment of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK.lld:pubmed
pubmed-article:15743210pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:15743210pubmed:publicationTypeResearch Support, U.S. Gov't, P.H.S.lld:pubmed
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