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Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.

Abstract：

:Indolic 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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Chauvignac C,Miller CN,Srivastava SK,Lewis JW,Husbands SM,Traynor JR

doi

10.1021/jm049172n

keywords:

subject

Has Abstract

pub_date

2005-03-10 00:00:00

pages

1676-9

issue

5

eissn

0022-2623

issn

1520-4804

journal_volume

48

pub_type

杂志文章

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