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| COCAETHYLENE - A NEUROPHARMACOLOGICALLY ACTIVE METABOLITE ASSOCIATED WITH CONCURRENT COCAINE-ETHANOL INGESTION |
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| Author(s): JATLOW P, ELSWORTH JD, BRADBERRY CW, WINGER G, TAYLOR JR, RUSSELL R, ROTH RH |
| Source: LIFE SCIENCES Volume: 48 Issue: 18 Pages: 1787-1794 Published: 1991 |
| Times Cited: 199 References: 39 |
| 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 [H-3]GBR 12395 to the dopamine reuptake complex, inhibition of [H-3]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. |
| Document Type: Article |
| Language: English |
| Reprint Address: JATLOW, P (reprint author), YALE UNIV, SCH MED, DEPT LAB MED, 333 CEDAR ST, NEW HAVEN, CT 06510 USA |
Addresses:
1. YALE UNIV, SCH MED, DEPT PSYCHIAT, NEW HAVEN, CT 06510 USA
2. YALE UNIV, SCH MED, DEPT PHARMACOL, NEW HAVEN, CT 06510 USA
3. UNIV MICHIGAN, SCH MED, DEPT PHARMACOL, ANN ARBOR, MI 48109 USA |
| Publisher: PERGAMON-ELSEVIER SCIENCE LTD, THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD, ENGLAND OX5 1GB |
| Subject Category: Medicine, Research & Experimental; Pharmacology & Pharmacy |
| IDS Number: FD957 |
| ISSN: 0024-3205 |
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