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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.