Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Neurology

Pain

m-Opioid receptor (OPRM1; MOR); cannabinoid CB1 receptor (CNR1)

SAR and mouse studies identified a bivalent dual MOR agonist and CNR1 antagonist that could be useful for treating pain. In cell culture, compounds containing an a-oxymorphamine MOR agonist pharmacophore linked to a CNR1 antagonist pharmacophore induced clustering and endocytosis of both receptors. In a mouse model for pain, intracerebroventricular and intrathecal injection of the bivalent compound decreased pain compared with injection of a monovalent MOR agonist control and did not lead to tolerance. Next steps could include further chemical optimization.

SciBX 6(28); doi:10.1038/scibx.2013.733
Published online July 25, 2013

Patent and licensing status undisclosed

Le Naour, M. et al. J. Med. Chem.;
published online June 4, 2013;
doi:10.1021/jm4005219
Contact: Philip S. Portoghese, University of Minnesota, Minneapolis, Minn.
e-mail:
porto001@umn.edu