Zherdev V P, Boyko S S, Mesonzhnik N V, Bastrygin D V
V. V. Zakusov Institute of Pharmacology, the Russian Academy of Medical Sciences, Moscow, Russia.
Bull Exp Biol Med. 2011 Jul;151(3):330-2. doi: 10.1007/s10517-011-1322-z.
Experiments on rats with measurements by HPLC-MS/MS showed that antipsychotic preparation dilept (N-caproyl-L-prolyl-L-tyrosine methyl ester) administered per os in doses of 40 and 200 mg/kg crossed the blood-brain barrier and was detected in rat brain (unchanged drug and its active metabolite N-caproyl-L-prolyl-L-tyrosine). The brain/plasma distribution coefficient for dilept was 2.0, for metabolite 0.5. No dose-concentration relationship was found, presumably because of the high dose of the drug transported from the blood to the brain not only by free diffusion, but also with participation of active carriers, whose number was limited.
通过HPLC-MS/MS测量对大鼠进行的实验表明，抗精神病制剂双硫仑（N-己酰基-L-脯氨酰-L-酪氨酸甲酯）以40和200mg/kg的剂量口服给药后穿过血脑屏障，并在大鼠脑中被检测到（未变化的药物及其活性代谢物N-己酰基-L-脯氨酰-L-酪氨酸）。双硫仑的脑/血浆分布系数为2.0，代谢物为0.5。未发现剂量-浓度关系，推测是因为从血液转运到大脑的药物高剂量不仅通过自由扩散，还通过活性载体的参与，而活性载体的数量是有限的。
