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MCL 1937.0: N-Substituted Derivatives of Morphinan and Uses Thereof

John Neumeyer, Ph.D., et al.

Background and Description

It is generally believed that opioid receptor agonists, particularly kappa (k) receptor agonists, can modulate the neurochemical and behavioral effects of cocaine. These effects may be caused by an inhibition or attenuation of the release of dopamine from dopaminergic neurons following cocaine administration. The present invention is based on the finding that nonselective k-agonists that can also induce m-receptor-mediated effects can decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective k-agonists. Several novel compounds having this activity are included in the invention. These compounds also have relatively low affinity for the d receptor and should therefore not produce the side effects associated with activity at this receptor.

Potential Commercial Uses

The compounds of the invention are potentially useful as treatments of cocaine abuse, possibly with fewer side effects than other drugs. The compounds can also be radioactively labeled with F-18 for positron emission tomography (PET) scanning, or with I-123 for single photon computed tomography (SPECT) imaging. Such labeled compounds could be used for imaging the localization and density of k receptors in the brain, and determining if this changes as a result of cocaine use or other stimuli.

Publication and Patent Status

McLean Hospital and the University of Rochester are the owners of U.S Patent Numbers 6,844,438 and 7,291,628 claiming this invention. (USPTO # 6,844,438 and 7,291,628)

Licenses Available

McLean Hospital is offering a worldwide exclusive license to this technology.

For more information, please contact:

Anne Ritter, Licensing Manager
Partners Research Ventures and Licensing
(617) 954-9529