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MCL 2245.0: Mixed Kappa/Mu Opioids and Uses Thereof

John L. Neumeyer, Ph.D.

Background and Description

It is generally believed that opioid receptor agonists, particularly kappa (κ) 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 certain κ-agonists that have mixed activity at both κ and mu (μ) opioid receptors may decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective κ-agonists. Therefore, mixed kappa/mu agonists appear to offer some advantages over selective κ-agonists as potential treatments for cocaine abuse and other disorders characterized by dopaminergic dysfunction or dysregulation. Several novel compounds having such activity are featured in the invention.

Potential Commercial Uses

Based on traditional structure-activity relationships that have pinpointed structural features important for receptor binding, the inventor has synthesized a novel series of mixed kappa/mu opioids having high affinity for the opioid receptors. The compounds of the invention are potentially useful as treatments of addiction to cocaine or other drugs, possibly with fewer side effects than other drugs. The compounds may also be effective therapeutics against pain and diseases characterized by dopamine dysregulation, such as schizophrenia, ADHD or depression.

Publication and Patent Status

McLean Hospital is the owner of U.S. Patent Number 7,271,173 claiming the compounds of this invention and methods of using these compounds to treat pain. (USPTO # 7,271,173)

Licenses Available

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

For more information, please contact:

David J. Glass, Ph.D.
Senior Associate Director, Technology Transfer
McLean Hospital Research Administration
115 Mill Street
Belmont, MA 02478-9106
(617) 855-3825 - tel
(617) 855-3745 - fax