A Simple and Efficient Method for the Preparation of Binaltrorphimine and Derivatives and determination of their  K  opioid antagonist selectivity | Zendy

Schmidhammer Helmut | Zendy; Smith Colin F. C. | Zendy

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A Simple and Efficient Method for the Preparation of Binaltrorphimine and Derivatives and determination of their K opioid antagonist selectivity

Author(s) -

Schmidhammer Helmut,

Smith Colin F. C.

Publication year - 1989

Publication title -

helvetica chimica acta

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.74

H-Index - 82

eISSN - 1522-2675

pISSN - 0018-019X

DOI - 10.1002/hlca.19890720408

Subject(s) - chemistry , selectivity , (+) naloxone , antagonist , naltrexone , potency , opioid antagonist , opioid , methylhydrazine , stereochemistry , combinatorial chemistry , medicinal chemistry , organic chemistry , receptor , biochemistry , in vitro , catalysis , phenylhydrazine

The bimorphinans 1 (binaltrorphimine), 3 , and 7 have been prepared by treatment of the parent morphinan‐6‐ones naltrexone ( 5 ), naloxone ( 4 ), and dihydrocodeinone ( 6 ), respectively, with N ‐methylhydrazine sulfate in AcOH at room temperature. Compound 3 showed opioid antagonist potency and selectivity for K receptors which were somewhat lower in comparison to 1 .

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