Synthesis and Biological Evaluation of 14‐Alkoxymorphinans. Part 10 . 14‐ O ‐Methyl derivatives of 5‐methylnaltrexone and 5‐methylnaloxone | Zendy

Schmidhammer Helmut | Zendy; Nussbaumer Christine | Zendy; Patel Dinesh | Zendy; Traynor John R. | Zendy

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Synthesis and Biological Evaluation of 14‐Alkoxymorphinans. Part 10 . 14‐ O ‐Methyl derivatives of 5‐methylnaltrexone and 5‐methylnaloxone

Author(s) -

Schmidhammer Helmut,

Nussbaumer Christine,

Patel Dinesh,

Traynor John R.

Publication year - 1994

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.19940770614

Subject(s) - chemistry , in vivo , antagonism , vas deferens , in vitro , agonist , ileum , stereochemistry , pharmacology , guinea pig , receptor , biochemistry , endocrinology , medicine , microbiology and biotechnology , biology

In several steps, 5, 14‐ O ‐dimethylnaltrexone ( 3 ) and 5, 14‐ O ‐dimethylnaloxone ( 4 ) were prepared starting from 5, 14‐ O ‐dimethyloxycodone ( 5 ). Compound 3 exhibited opioid agonism in vitro (guinea‐pig ileum and mouse vas deferens preparations) and antagonism in vivo (AcOH‐writhing test in mice), while compound 4 was found to be an agonist in vitro and in vivo .

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