Mixed Azines of Naloxone with Dihydromorphinone Derivatives | Zendy

Schmidhammer Helmut | Zendy; Kaspar Felizia | Zendy; Marki Arpad | Zendy; Borsodi Anna | Zendy

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Mixed Azines of Naloxone with Dihydromorphinone Derivatives

Author(s) -

Schmidhammer Helmut,

Kaspar Felizia,

Marki Arpad,

Borsodi Anna

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.19940770412

Subject(s) - chemistry , oxymorphone , agonist , (+) naloxone , partial agonist , morphine , potency , in vivo , opioid , pharmacology , stereochemistry , in vitro , receptor , biochemistry , medicine , oxycodone , microbiology and biotechnology , biology

The mixed azines 4 and 5 were prepared by reaction of naloxazone ( 2 ) with either oxymorphone ( 6 ) or 14‐ O ‐methyloxymorphone ( 7 ) and tested in vitro using opioid receptor binding assays and in vivo using the AcOH‐writhing test in mice. Compound 4 was found to be a partial agonist, while compound 5 was a potent opioid agonist with higher potency than morphine.

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