Cocaethylene: a neuropharmacologically active metabolite associated with concurrent cocaine-ethanol ingestion.

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 12935 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.

journal_name

Life Sci

journal_title

Life sciences

authors

Jatlow P,Elsworth JD,Bradberry CW,Winger G,Taylor JR,Russell R,Roth RH

doi

10.1016/0024-3205(91)90217-y

subject

Has Abstract

pub_date

1991-01-01 00:00:00

pages

1787-94

issue

18

eissn

0024-3205

issn

1879-0631

pii

0024-3205(91)90217-Y

journal_volume

48

pub_type

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