| Literature DB >> 11784158 |
Sanjay K Srivastava1, Stephen M Husbands, Mario D Aceto, Carl N Miller, John R Traynor, John W Lewis.
Abstract
A new method for the preparation of N-benzylpyrrolomorphinans has been developed. Thus Michael reaction of the benzylimines of oxycodones and oxymorphones with nitrostyrenes gave a series of 4'-aryl-N-benzylpyrrolomorphinans. These were selective delta antagonists of much higher in vitro potency (with 5a having K(e) delta = <1 nM) than their binding affinities predicted. In mice in vivo assays 5a showed good delta antagonist activity in the anti-writhing analgesic assay and also inhibited delta agonist-induced convulsant activity.Entities:
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Year: 2002 PMID： 11784158 DOI： 10.1021/jm010841w
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446