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新麻醉药静松灵生物转化的研究
引用本文:郭联庆,黄如衡.新麻醉药静松灵生物转化的研究[J].药学学报,1990,25(2):95-100.
作者姓名:郭联庆  黄如衡
作者单位:军事医学科学院毒物药物研究昕,军事医学科学院毒物药物研究昕 北京 100850,北京 100850
摘    要:静松灵2-(2,4-二甲基苯胺基)-4,5-二氢噻唑,XT]是国内合成的麻醉物,经ip给药后,从大鼠尿中分离、纯化、鉴定了四个代谢产物。MB1即XT原形;MB3及MA2互为异构体,分别为2位、4位甲基氧化为羧基的产物;MA1则4位甲基氧化为羧基,二氢噻唑环中41位亚甲基氧化为羰基。初步实验表明:代谢产物MB3,MA2,MA1的药效与毒性均远低于原形药,大鼠与小鼠对XT的转化机制相近,但也存在种属的差异。

关 键 词:静松灵  麻醉药  生物转化
收稿时间:1988-10-31

STUDIES ON BIOTRANSFORMATION OF JING SONG LING, A NEW ANESTHETIC
LQ Guo and RH Huang.STUDIES ON BIOTRANSFORMATION OF JING SONG LING, A NEW ANESTHETIC[J].Acta Pharmaceutica Sinica,1990,25(2):95-100.
Authors:LQ Guo and RH Huang
Institution:Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing.
Abstract:Jing song ling (2,4-xyJidinothiazoline, XT) is a new anestheticagent for veterinary uses in China. From urine of rats given the drug three metabolites (MA_1, MA_2 and MB_3) were isolated with structures shown in page 98 in addition to the parent compound (MB_1). Preliminary observations showed that the toxicity and pharmacological activity of MB_3, MA_2 and MA_1 decreased significantly compared with the parent drug XT. Species difference of biotransformation of XT between rat and mouse was also observed.
Keywords:2  4-Xylidinothiazoline  Anesthetic  Biotransformation
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