新麻醉药静松灵生物转化的研究

STUDIES ON BIOTRANSFORMATION OF JING SONG LING, A NEW ANESTHETIC

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。

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 (MA₁, MA₂ and MB₃) were isolated with structures shown in page 98 in addition to the parent compound (MB₁). Preliminary observations showed that the toxicity and pharmacological activity of MB₃, MA₂ and MA₁ decreased significantly compared with the parent drug XT. Species difference of biotransformation of XT between rat and mouse was also observed.