Mizuchi A, Kitagawa N, Miyachi Y
Psychopharmacology (Berl). 1983;81(3):195-8. doi: 10.1007/BF00427261.
Sensitive and specific radioimmunoassays for both sultopride and sulpiride were developed. Using these radioimmunoassays, the regional distributions of sultopride and sulpiride in rat brain after intraperitoneal administration were investigated. Although relatively small amounts of both drugs were detected in the brain, sultopride appears to pass the blood-brain barrier more easily than sulpiride. Relatively high concentrations of sultopride were seen in hypothalamus, striatum, the mesolimbic area and hippocampus, while sulpiride accumulated mainly in brain areas such as hypothalamus, medulla oblongata and cerebellum, where the blood-brain barrier is less effective. Both drugs seem to be concentrated by the pituitary and pineal body. These differences between sultopride and sulpiride in penetration to the brain may depend on their different lipid solubilities, since sultopride has a higher lipid solubility compared with sulpiride.
开发了针对舒托必利和硫必利的灵敏且特异的放射免疫分析方法。使用这些放射免疫分析方法,研究了腹腔注射后舒托必利和硫必利在大鼠脑中的区域分布。尽管在脑中检测到的两种药物量相对较少,但舒托必利似乎比硫必利更容易通过血脑屏障。在下丘脑、纹状体、中脑边缘区和海马体中观察到相对较高浓度的舒托必利,而硫必利主要积聚在血脑屏障作用较弱的脑区,如下丘脑、延髓和小脑。两种药物似乎都在垂体和松果体中富集。舒托必利和硫必利在脑内渗透方面的这些差异可能取决于它们不同的脂溶性,因为与硫必利相比,舒托必利具有更高的脂溶性。