Monomeric and Dimeric Heterocycles for Treating Cocaine Abuse
Section: For Industry
Categories: "Neurodegenerative Therapeutics"
Reference #: 1999-040
OTC Contact: Ruchika Nijhara, Ph.D. (Directory Information | Send a Message)
Description
Cocaine remains one of the most prevalent drugs of abuse in the world, in part because of its highly addictive properties. Monomeric and dimeric heterocycles, discovered by Georgetown researchers, mimic some of the physiological effects of cocaine, but do not have cocaine’s potential for abuse. In particular, certain piperidine ring containing compounds have demonstrated high affinity for the dopamine transporter (DAT) and inhibition of dopamine uptake. Preliminary self-administration studies in rats have revealed that specific new compounds of the invention do not exhibit the positive reinforcing properties of cocaine. These new agents represent a novel approach to therapeutic leads for treating cocaine abuse.
Applications
- Therapeutic agents for the treatment of cocaine addiction
- Research tools to probe dopamine transporter (DAT) binding
Advantages
- Dopamine inhibitors of the invention lacked the addictive effects of cocaine in self-administration studies of rats.
- These analogs may be used for treating cocaine addiction in a manner similar to how methadone is used in the treatment of opiate abuse.
Stage of Development
In vitro assays validate activity and potency and preliminary animal studies show a lack of addictive properties for some compounds.Relevant Publications
Kozikowski, A.P.; Araldi, G.L.; Boja, J.; Meil, W.M.; Johnson, K.M.; Flippen-Anderson, J.L.; George, C.; Saiah, E. J. Med. Chem. 1998, 41, 1962-1969.
INVENTORS: Alan P. Kozikowski, et al.
Patent Status
U.S. Patent No. 6,440,996, Filed October 7, 1999, Issued August 27, 2002
