European Journal of Pharmacology 1990-08-10

New, potent cocaine analogs: ligand binding and transport studies in rat striatum.

J W Boja, F I Carroll, M A Rahman, A Philip, A H Lewin, M J Kuhar

文献索引：Eur. J. Pharmacol. 184(2-3) , 329-32, (1990)

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摘要

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.