Synthesis and biological evaluation of 14‐alkoxymorphinans. Part 7.  14,14′‐dimethoxy analogues of norbinaltorphimine: Synthesis and determination of their χ opioid antagonist selectivity | Zendy

Schmidhammer Helmut | Zendy; Ganglbauer Ernst | Zendy; Mitterdorfer Jörg | Zendy; Rollinger Judith M. | Zendy; Smith Colin F. C. | Zendy

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Synthesis and biological evaluation of 14‐alkoxymorphinans. Part 7. 14,14′‐dimethoxy analogues of norbinaltorphimine: Synthesis and determination of their χ opioid antagonist selectivity

Author(s) -

Schmidhammer Helmut,

Ganglbauer Ernst,

Mitterdorfer Jörg,

Rollinger Judith M.,

Smith Colin F. C.

Publication year - 1990

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.19900730622

Subject(s) - chemistry , selectivity , antagonist , combinatorial chemistry , stereochemistry , opioid receptor , receptor , pharmacology , organic chemistry , biochemistry , catalysis , medicine

The bimorphinans 6 and 7 have been prepared from 14 ‐ O ‐methylnaloxone ( 2 ) and 14‐ O ‐methylnaltrexone ( 3 ), respectively. The known compounds 2 and 3 were synthesized by a different route than the route described. Bimorphinan 7 possessed a similar χ receptor affinity to norbinaltorphimine ( 1 ) but had a reduced selectivity due to marked increases in μ and δ receptor affinity. Bimorphinan 6 was both a less selective and less potent χ antagonist than 1 .

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