New Derivative of Dextromethorphan for Use in Neuronal Therapy

This invention describes a derivative of dextromethorphan, which is a non-competitive inhibitor of the nicotinic acetylcholine receptor. Dextromethorphan is an antitussive drug used as one of the active ingredients to prevent coughs in many over-the-counter cold and cough medicines. It has also found other uses in medicine, ranging from pain relief to psychological applications. The disclosed compound may display attractive properties compared to the closely related dextromethorphan or other drugs currently in use as non-competitive inhibitors of the nicotinic acetylcholine receptors, including extended receptor inhibition and reduced side effects.

The nicotine acetylcholine receptor is a ligand gated ion channel. These receptors specifically control rapid permeation of cations through the postsynaptic cell membrane, and are key targets in drug discovery for a number of diseases such as Alzheimer's and Parkinson's disease. This superfamily of receptor proteins is separated into the nicotinic receptor superfamily (muscular and neuronal nicotinic), the excitatory amino acid superfamily, and the ATP purinergic ligand gated ion channels, and they differ only in the number of transmembrane domains found in each subunit. This newly discovered derivative of dextromethorphan may have potential therapeutic use for several conditions involving these nicotinic acetylcholine receptors.

Development Stage:
Early stage


Irving Wainer (NIA)  ➽ more inventions...

Intellectual Property:
U.S. Pat: 7,749,984 issued 2010-07-06
US Application No. 10/820,809

K Jozwiak et al. Displacement and non-linear chromatographic techniques in the investigation of the interaction of noncompetitive inhibitors with an immobilized alpha3beta4 nicotinic acetylcholine receptor liquid chromatographic stationary phase. Anal Chem. 2002 Sep 15;74(18):4618-4624. PubMed abs

Collaboration Opportunity:

The National Institute on Aging, Laboratory of Clinical Investigation, is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize a series of noncompetitive inhibitors of neuronal nicotinic acetylcholine receptors based upon the dextromethorphan and levomethorphan scaffolds including molecular modeling and synthesis of new derivatives, receptor binding and occupancy studies and non-competitive inhibition of nicotinic acetylcholine receptors subtypes and related ligand gated ion channels. Please contact Nicole Darack, Ph.D. at 301-435-3101 or for more information.

Licensing Contact:
Richard Girards,
Phone: 240-276-5360

OTT Reference No: E-158-2003/1
Updated: Nov 4, 2009