Ion cluster techniques in drug metabolism: use of a mixture of labeled and unlabeled cocaine to facilitate metabolite identification.
Ion cluster techniques in drug metabolism: use of a mixture of labeled and unlabeled cocaine to facilitate metabolite identification.
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药物代谢中的离子簇技术：使用标记和未标记可卡因的混合物来促进代谢物识别。
DOI：
10.1093/jat/10.4.150
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发表时间：
1986
影响因子：
2.5
通讯作者：
Lutz,T
中科院分区：
文献类型：
--
作者：
Jindal,SP;Lutz,T
描述了大鼠中的可卡因处置研究。使用可卡因、可卡因-d3、可卡因-14C和可卡因-3H的混合物作为剂量。收集尿液，用有机溶剂萃取，并使用 NPLC 和 TLC 收集级分。放射性可卡因可用于分离代谢物，而氘标记的可卡因可产生人工同位素簇，通过气相色谱/质谱法对代谢物进行特异性鉴定。发现苯甲酰爱康宁、芽子碱甲酯、爱康定、去甲可卡因、N-羟基去甲可卡因、羟基可卡因和羟基甲氧基可卡因是主要代谢物，而芽子碱、苯甲酰去甲爱康宁和可卡因-N-氧化物似乎以微量存在。初步鉴定为二甲氧基羟基可卡因。其中几种新发现的可卡因代谢物浓度很高，可能会导致可卡因的毒性作用。
Cocaine disposition studies in the rat are described. A mixture of cocaine, cocaine-d3, cocaine-14C, and cocaine-3H was used as a dose. The urine was collected, extracted with organic solvents, and fractions collected using NPLC and TLC. The radioactive cocaine was useful in the separation of metabolites while the deuterium-labeled cocaine, creating an artificial isotopic cluster, provided specific identification of the metabolites by gas chromatography/mass spectrometry. Benzoylecgonine, ecgoninemethylester, ecgonidine, norcocaine, N-hydroxynorcocaine, hydroxycocaine, and hydroxymethoxycocaine were found to be the major metabolites, while ecgonine, benzoylnorecgonine, and cocaine-N-oxide seemed to be present in trace amounts. Dimethoxyhydroxy cocaine was tentatively identified. Several of these newly identified metabolites of cocaine were present in significant concentrations and could contribute to the toxic effects of cocaine.