ALCOHOL RECEPTORS AND METHODS TO DEVELOP COMPOUNDS FOR THE TREATMENT OF ALCOHOLISM AND ANXIETY
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UCLA Technology Available For Licensing |
BACKGROUND:
Despite the ubiquity of alcohol consumption, the molecular mechanism by which it exerts its physiological effects has remained elusive. Previous research into the molecular interactions of alcohol with benzodiazepines led to the discovery of Ro15-4513, a structural analog of the benzodiazepine antagonist flumazenil, as an effective alcohol antidote which initially showed promise as a useful compound to treat alcohol overdoses. However, the short half life Ro15-4513, along with the fact that Ro15-4513 binds many other targets and therefore has side-effects, has stymied efforts to commercialize Ro15-4513 as an antidote for alcohol. Methods to facilitate drug discovery for the treatment of alcoholism is vital to identify new lead compounds to treat alcoholism and anxiety.
INNOVATION:
Investigators at the UCLA Department of Molecular and Medical Pharmacology have identified subtypes of GABAA receptors that have a previously unrecognized high affinity alcohol/Ro15-4513 binding pocket. Compounds that bind to this site and mimic the effects of alcohol could be extremely valuable, which could yield the benefits of moderate alcohol consumption. Potential benefits include anxiolytic, sedative, anticonvulsant, and mood-enhancing effects. The invention also describes a method that can be used to identify compounds that mimic or modulate the ethanol response of a subject. Together with high-throughput methods to screen large compound libraries, this new approach can be used to find compounds that could be developed into new drugs.
POTENTIAL APPLICATIONS
- Identify new compounds to be used in the pharmacotherapy of alcoholism and acute alcohol intoxication.
- Discover therapeutics that replicates the anti-anxiety, anti-depressive effects produced by low doses of alcohol.
- Find agonists of the receptor that duplicate the anticonvulsive actions of alcohol, which can be used in treating convulsions and epilepsy.
ADVANTAGES
- No known drugs marketed today harness the positive effects of alcohol, and there are no alcohol antidotes on the market.
- The ethanol binding site is presently unutilized in current drug therapies.
- Specificity for this target can reduce side effects that are common in current anxiolytic and sedative drugs, and may be less addictive.
DEVELOPMENT-TO-DATE:
Receptors have been shown to respond to alcohol concentrations that mirror alcohol effects in humans. Several lead compounds have been identified from the information gained from the present discovery.
For additional technical details and current licensing
availability,
please contact the following UCLA office:
UCLA Office of Intellectual Property
11000 Kinross Avenue, Suite #200
Los Angeles, CA 90095-7231
Tel: 310-794-0558 Fax: 310-794-0638
email: ncd@research.ucla.edu
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NCD URL: http://www.research.ucla.edu/tech/ucla05-458.htm
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UCLA Technologies Available for
Licensing
http://www.research.ucla.edu/oipa/industry
Copyright © 2007 The Regents of the
University of California.
keywords: alcohol receptors, ethanol, gaba, benzodiazepine, flumazenil, alcoholism, anxiety, sedative, anticonvulsant
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