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大白鼠一次给不同剂量的美散痛后,测量各时间内它在脑中及血浆中浓度与镇痛效果之间的关系。随着剂量的增加,镇痛面积和最大镇痛效应(热板法),以及在脑内,血浆中的浓度均增加。在最大镇痛作用时,美散痛的镇痛效应定量地与它在脑内及血浆中的浓度有关。美散痛在肝内通过 N-甲基化,环化,羟基化和葡萄糖醛酸化进行代谢。美散痛有镇痛作用,其代谢物均无镇痛作用。本文用 HPLC 分析~(14)C-美散痛后,在脑中美散痛占所有含~(14)C
Rats once to different doses of the United States pain, the measurement of each time it in the brain and plasma concentration and the relationship between the analgesic effect. As the dose increased, the analgesic area and maximal analgesic effect (hot plate method), as well as in the brain, increased in plasma. The analgesic effect of Parthenolide is quantitatively related to its concentration in the brain and plasma at maximum analgesia. Bleeding pain is metabolized in the liver by N-methylation, cyclization, hydroxylation and glucuronidation. There are analgesic effects of the United States pain, the metabolites have no analgesic effect. In this paper, HPLC analysis of ~ (14) C-US pain, the United States in the brain of all the pain containing ~ (14) C