Cocaethylene: A neuropharmacologically active metabolite assciated with concurrent cocaine-ethanol ingestion

P. Jatlow, J. D. Elsworth, C. W. Bradberry, G. Winger, J. R. Taylor, R. Russell, R. H. Roth

Research output: Contribution to journalArticlepeer-review

212 Scopus citations

Abstract

High concentrations of cocaethylene (EC), the ethyl ester of benzoylecgonine, were measured in the blood of individuals who had concurrently used cocaine and ethanol. Since the powerful reinforcing effects of cocaine appear to be dependent on inhibition of dopamine reuptake in brain, we compared the effects of EC on the dopamine uptake system and its behavioral effects with those of cocaine. EC was equipotent to cocaine with respect to inhibition of binding of [3H]GBR 12395 to the dopamine reuptake complex, inhibition of [3H]dopamine uptake into synaptosomes and in its ability to increase extracellular dopamine concentration in the nucleus accumbens following its systemic administration to rats. Moreover, in rats, EC and cocaine each increased locomotor activity and rearing to the same extent following i.p. administration. In self-administration studies in primates, EC was approximately equipotent to cocaine in maintaining responding. The in vivo formation of this active, transesterified ethyl homolog of cocaine may contribute to the effects and consequences of combined cocaine and ethanol abuse.

Original languageEnglish (US)
Pages (from-to)1787-1794
Number of pages8
JournalLife Sciences
Volume48
Issue number18
DOIs
StatePublished - 1991
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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