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给大鼠灌胃~3H-东莨菪碱与~3H-樟柳碱后,吸收都好,但前者的吸收比后者更快更完全。静脉注射后,前者的T1/2α为11分钟,T1/2β为95分钟,后者的T1/2α为13分钟,T1/2β为70分钟。静脉注射后二者的组织浓度均以肺与肾最高,脑内的浓度都比血浆内者高。两药在脑的分布形式相似,以纹状体、大脑皮层及海马较多,膈区和间脑次之,低位脑干和小脑较低。虽然两药的血浆浓度相似,但在脑内各区的分布~3H-东莨菪碱明显高于~3H-樟柳碱。 两药静脉注射后,仅很小部分原形药从尿及粪排出,大部分以转化形式排出。两药都可被大鼠肝和血浆所转化,家兔的肝、肾和血浆也有这种活性,而且更强。~3H-东莨菪碱的转化速度明显地比~3H-樟柳碱快。 ~3H-东莨菪碱与~3H-樟柳碱在代谢上的差异可能与后者托品酸部分多一羟基因而极性较大有关。
After rats were administered ~ 3H-scopolamine and ~ 3H-anisodine, the absorption is good, but the former’s absorption faster and more completely than the latter. After iv injection, T1 / 2α for the former was 11 minutes, T1 / 2β for 95 minutes, the latter for T1 / 2α for 13 minutes and T1 / 2β for 70 minutes. Intravenous injection of both tissue concentrations were the highest in lung and kidney, brain concentrations were higher than those in plasma. The distribution of two drugs in the brain in the form of similar to the striatum, cerebral cortex and hippocampus more, followed by the diaphragm and the brain, low brain stem and cerebellum lower. Although plasma concentrations of the two drugs are similar, the distribution of ~ 3H-scopolamine in the brain regions was significantly higher than that of ~ 3H-anisodine. After intravenous injection of two drugs, only a small part of the prototype drug excreted from the urine and excrement, most of the conversion form of discharge. Both drugs can be transformed by rat liver and plasma, and the liver, kidney and plasma of rabbits also have this activity and are stronger. ~ 3H-scopolamine conversion rate was significantly faster than ~ 3H-anisodine. ~ 3H-scopolamine and ~ 3H-anisodine in the metabolic differences may be related to the latter part of the tropic acid hydroxyl and thus more polar polarity.