^3H—川芎嗪在动物体内分布与排泄的定量研究

Quantitative Study on the Distribution and Excretion of ~3H-Tetramethyl-Pyrazine in Mice

用~3H标记川芎嗪作为示踪剂,经小鼠尾静脉注入其体内,在24h内的10个时相测量其15种器官组织450份样品的示踪剂含量,以进一步观察~3H—川芎嗪在动物体内的分布、排泄情况,探讨中药川芎的药性归经理论。实验结果表明,小鼠体内对~3H—川芎嗪的敏感靶器官是消化系统,尤以肝脏、胆汁和小肠最明显。~3H—川芎嗪还大量分布于肺脏并可透过血脑、血睾屏障稳定而持久地存在;绝大部分经肾脏从尿中排出体外。实验结果与中药川芎的归经记载十分符合。

32 mice (NIH, male, 16-18g) were used in this experiment. ~3H-Tetramethylpyrazine was used as a tracer agent. It (370KBq/gram body weight) was injected into the caudal vein of the mice and the tracing time was from one minute to 24 hours. The mice were divided into 10 groups according to the different tracing time. The content of the tracer agent in 15 organs and tissues in each mouse (the total number of the specimens was 450) was measured by the Beckman LS 8501 liquid Scientillation Counter, with which quantitative observations of the distribution and excretion of ~3H-Tetramethyl-Pyrazine in mice were done. The results of the experiment suggested that the organs sensitive to ~3H-Tetramethyl-Pyrazine involved the digestive system, especially the liver, bile and the small intestines. It was also distributed in the brain, the lung and the testis. The ~3H-Tetramethyl-Pyrazine may pass through the blood-cerebral barrier and the blood-testis barrier, and it is excreted mainly through the kidney. Preiiminary research was done the mechanism of 'Channel Tropism' of Tetramethyl-Pyrazine.