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New, potent cocaine analogs: ligand binding and transport studies in rat striatum
J W Boja1, F I Carroll, M A Rahman
1Neuroscience Branch, Addiction Research Center, National Institute on Drug Abuse, Baltimore, MD 21224.
European Journal of Pharmacology
|August 10, 1990
Abstract:
Two potent cocaine analogs have been developed that have the highest known affinities for the cocaine binding site in rat striatum. Both 3 beta-(4-chlorophenyl)- (RTI-COC-31) and 3 beta-(4-methylphenyl)-tropane-2-carboxylic acid methyl ester (RTI-COC-32) compete for [3H]WIN 35,428 and [3H]mazindol binding with a IC50 that is 100 times more potent than that of (-) cocaine. Additionally, these compounds inhibit [3H]dopamine uptake with a similar, high potency. These results may lead to the development of high affinity probes for the cocaine binding site.