N-Cubylmethyl substituted morphinoids as novel narcotic antagonists
Journal
Bioorganic and Medicinal Chemistry
Journal Volume
4
Journal Issue
1
Pages
73-80
Date Issued
1996
Author(s)
Abstract
N-Cubylmethylnormorphine (1) and N-cubylmethylnoroxymorphone (2) have been synthesized and found to be more potent ligands at the mu and kappa opioid receptors than morphine and oxymorphone respectively. In the guinea-pig ileum preparation, compounds 1 and 2 were characterized as opioid mu antagonists (Ke = 68 and 16 nM, respectively). Compound 2 also showed effective kappa-antagonism (Ke = 22 nM). The narcotic antagonism activity of 1 has been confirmed by in vivo assays.
Type
journal article