Differential relationships among dopamine transporter affinities and stimulant potencies of various uptake inhibitors

Sari Izenwasser, Philip Terry, Brett Heller, Jeffrey M. Witkin, Jonathan L. Katz

Research output: Contribution to journalArticlepeer-review

61 Scopus citations


Binding to the dopamine transporter and inhibiting dopamine reuptake are considered important factors in regulating behavioral effects of cocaine. One prominent behavioral effect of cocaine and other dopamine uptake inhibitors is the stimulation of locomotor activity. To examine the relationship between action at the dopamine transporter and behavior, the displacement of [3H]WIN 35,428 (CFT naphthalene sulfate; 2-β-carbomethoxy-3-β-(4-fluorophenyl)tropane-1,5-naphthalene disulfonate) binding in rat caudate putamen by cocaine and other uptake inhibitors was compared with stimulation of mouse locomotor activity. There was a significant correlation among affinities for binding and potencies for stimulating activity for cocaine and structurally similar compounds. For structurally dissimilar uptake inhibitors, however, there was no significant correlations among potencies for stimulation of activity and affinity for displacement of [3H]WIN 35,428 binding. These findings provide evidence that cocaine analogs may bind to the dopamine transporter in a manner that is fundamentally different from that for structurally dissimilar uptake inhibitors.

Original languageEnglish (US)
Pages (from-to)277-283
Number of pages7
JournalEuropean Journal of Pharmacology
Issue number3
StatePublished - Oct 3 1994
Externally publishedYes


  • Cocaine
  • Dopamine transporter
  • Dopamine uptake

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology


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