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

Eur J Pharmacol. 1990 Aug 10;184(2-3):329-32. doi: 10.1016/0014-2999(90)90627-i.


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.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Binding, Competitive
  • Biological Transport
  • Cocaine / analogs & derivatives*
  • Cocaine / metabolism
  • Corpus Striatum / metabolism*
  • Dopamine / metabolism
  • In Vitro Techniques
  • Radioligand Assay
  • Rats
  • Synaptosomes / drug effects
  • Synaptosomes / metabolism


  • 3-(4-chlorophenyl)tropane-2-carboxylic acid methyl ester
  • RTI-COC 32
  • (1R-(exo,exo))-3-(4-fluorophenyl)-8-methyl-8- azabicyclo(3.2.1)octane-2-carboxylic acid, methyl ester
  • troparil
  • Cocaine
  • Dopamine