Dean R A, Christian C D, Sample R H, Bosron W F
Department of Pathology, Indiana University School of Medicine, Indianapolis 46202-5122.
FASEB J. 1991 Sep;5(12):2735-9. doi: 10.1096/fasebj.5.12.1916095.
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 carboxyl-esterase 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.
据报道，在同时使用可卡因和乙醇的个体中出现了一种新的、具有药理活性的可卡因代谢物——乙基可卡因。乙基可卡因的形成可能导致这两种药物的共同滥用以及这种行为明显的危险性。我们已经鉴定出一种非特异性羧基酯酶，在乙醇存在的情况下，它能催化可卡因的乙基酯交换反应生成乙基可卡因。在没有乙醇的情况下，这种人肝脏酯酶催化可卡因水解生成苯甲酰芽子碱，一种作为精神运动兴奋剂无活性的代谢物。还描述了另一种人肝脏酯酶。这种酶催化可卡因水解生成芽子碱甲酯，同样作为兴奋剂无活性。这两种肝脏酯酶可能在调节可卡因的代谢失活中发挥重要作用。
