The dopamine transporter (DAT) plays an important role in pathophysiological processes in the central nervous system. In cocaine addiction, binding of cocaine to the DAT and consequent blockage of dopamine uptake appears to be related to the reinforcing properties of the drug. Also associated with the transport function is concentration of neurotoxic chemicals in dopaminergic neurons which is implicated in Parkinson’s disease. Potent, yet selective ligands for the DAT have potential for in vivo monitoring of primary targets of cocaine in the brain, for the characterization of cocaine binding sites, for pharmacotherapeutic agents for the treatment of cocaine addiction and for monitoring of Parkinson’s disease. Novel compounds have been developed in a few different molecular templates. These compounds have exhibited neuropharmacological activity with respect to their interaction with the dopamine transporter, the serotonin transporter (SERT) and the norepinepherine transporter (NET). Preferred lead compounds exhibit low nanomolar activity with respect to the DAT, and high differential binding activity with respect to the DAT compared with that for the SERT and for the NET. These compounds have utility in treating central nervous system disorders, including cocaine addiction, depression, and Parkinson’s disease.
Commercial Applications
· Medications for neurodegenerative diseases
· Treatment of Addiction
Patent Status:
U.S. patent number 6,995,268 is available for exclusive licensing.
Tech ID
00-513