Zhao M, Huang R H
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing.
Yao Xue Xue Bao. 1990;25(11):801-6.
Similar to eserine, Cui Xing Ning [CXN),5-(1,3,3-trimethylindoline) N, N-dimethyl carbamate] is a choline esterase (ChE) inhibitor. The biotransformation of CXN, which had been studied in vivo and in vitro unsuccessfully, was studied by using isolated perfused rat liver (IPL) method. Six metabolites of CXN from the perfusate were separated by HPLC, and identified with MS, 1HNMR or compared with the authentic compounds. Metabolite I is unchanged CXN, the other are oxidized metabolites. Most of the metabolites lost their activities of ChE inhibition strikingly except metabolite III which retained the 2-position unchanged. The toxicities of some metabolites (II,V) decreased obviously.
与毒扁豆碱类似,崔兴宁[CXN,5-(1,3,3-三甲基吲哚啉)N,N-二甲基氨基甲酸酯]是一种胆碱酯酶(ChE)抑制剂。此前在体内和体外对CXN的生物转化研究均未成功,此次采用离体灌注大鼠肝脏(IPL)方法对其进行研究。通过高效液相色谱(HPLC)从灌注液中分离出CXN的六种代谢产物,并用质谱(MS)、核磁共振氢谱(1HNMR)进行鉴定或与标准化合物进行比较。代谢产物I为未变化的CXN,其他为氧化代谢产物。除2位未变化的代谢产物III外,大多数代谢产物的ChE抑制活性显著丧失。一些代谢产物(II、V)的毒性明显降低。