MIXED AZINES OF NALOXONE WITH DIHYDROMORPHINONE DERIVATIVES

Authors
SCHMIDHAMMER H KASPAR F MARKI A BORSODI A
Citation
H. Schmidhammer et al., MIXED AZINES OF NALOXONE WITH DIHYDROMORPHINONE DERIVATIVES, Helvetica Chimica Acta, 77(4), 1994, pp. 999-1002
Citations number
19
Categorie Soggetti
Chemistry
Journal title
Helvetica Chimica Acta → ACNP
ISSN journal
0018019X
Volume
77
Issue
4
Year of publication
1994
Pages
999 - 1002
Database
ISI
SICI code
0018-019X(1994)77:4<999:MAONWD>2.0.ZU;2-7
Abstract
The mixed azines 4 and 5 were prepared by reaction of naloxazone (2) w ith 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.