DESIGN AND SYNTHESIS OF 10-OXO DERIVATIVE OF N-CYCLOPROPYLMETHYL (-)-6-BETA-ACETYLTHIODIHYDRONORMORPHINE, A POTENTIALLY KAPPA-SELECTIVE OPIOID RECEPTOR-LIGAND

Authors
SAGARA T OZAWA S KUSHIYAMA E KOIKE K TAKAYANAGI I KANEMATSU K
Citation
T. Sagara et al., DESIGN AND SYNTHESIS OF 10-OXO DERIVATIVE OF N-CYCLOPROPYLMETHYL (-)-6-BETA-ACETYLTHIODIHYDRONORMORPHINE, A POTENTIALLY KAPPA-SELECTIVE OPIOID RECEPTOR-LIGAND, Bioorganic & medicinal chemistry letters, 5(14), 1995, pp. 1505-1508
Citations number
7
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
14
Year of publication
1995
Pages
1505 - 1508
Database
ISI
SICI code
0960-894X(1995)5:14<1505:DASO1D>2.0.ZU;2-C
Abstract
The design and synthesis of 10-oxo derivative of N-cyclopropylmethyl-( -)-6 beta-acetylthio dihydronormorphine (4) are described. The result of pharmacological assays indicate that compound 4 acts as a mu-opioid receptor antagonist and kappa-opioid receptor agonist which is sugges ted to be more potent analgesic action than that of 1 and morphine thr ough an activation of kappa-opioid receptors.