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Human liver cocaine esterases: ethanol‐mediated formation of ethylcocaine
Author(s) -
Dean Robert A.,
Christian Charles D.,
Sample R. H. Barry,
Bosron William F.
Publication year - 1991
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.5.12.1916095
Subject(s) - ethanol , chemistry , pharmacology , human liver , medicine , biochemistry , in vitro
A new, pharmacologically active metabolite of cocaine, ethylcocaine, has been reported in individuals after concurrent use of cocaine and ethanol. Formation of ethylcocaine may contribute to the common coabuse of these two drugs and the apparent danger of this practice. We have identified a nonspecific carboxylesterase that catalyzes the ethyl transesterification of cocaine to ethylcocaine in the presence of ethanol. In the absence of ethanol, this human liver esterase catalyzes the hydrolysis of cocaine to benzoylecgonine, a metabolite that is inactive as a psychomotor stimulant. A second human liver esterase is also described. This enzyme catalyzes hydrolysis of cocaine to ecgonine methyl ester, also inactive as a stimulant. These two liver esterases may play important roles in regulating the metabolic inactivation of cocaine.—Dean, R. A.; Christian, C. D.; Sample, R. H. B.; Bosron, W. F. Human liver cocaine enterases: ethanol‐mediated formation of ethylcocaine. FASEB J. 5: 2735‐2739; 1991.