Przuntek H, Westarp M E, Vohl M L, Gerlach M, Jutzi P, Wekerle H
Neuropharmacology. 1987 Feb-Mar;26(2-3):255-60. doi: 10.1016/0028-3908(87)90216-4.
The effect of methotrexate and of silyl-methotrexate were compared in the treatment of experimental allergic encephalomyelitis (EAE) mediated by T-line lymphocytes. It was demonstrated that, during the first three days after cell transfer, no difference between methotrexate and its silyl derivative could be seen. At a time when the cytotoxic lymphoblasts must have penetrated the blood brain barrier, only silyl methotrexate was able to prevent severe paralysis and death of the animals. It is suggested that the effect of N,N,O,O-Tetrakis (t-butyldimethylsilyl)-methotrexate, (N-4-N-(2,3-bis-t-butyldimethylsilyl-amino-6-pteridinyl-methyl)- methylamino-benzoyl-glutamic acid-bis-(t-butyldimethylsilyl)-ester), depends on the increased lipid solubility and permeability of the blood brain barrier of silylated drugs.
比较了甲氨蝶呤和甲硅烷基甲氨蝶呤在治疗由T淋巴细胞介导的实验性变应性脑脊髓炎（EAE）中的效果。结果表明，在细胞转移后的头三天，甲氨蝶呤与其甲硅烷基衍生物之间没有差异。当细胞毒性淋巴母细胞一定已经穿透血脑屏障时，只有甲硅烷基甲氨蝶呤能够预防动物出现严重麻痹和死亡。有人提出，N，N，O，O-四（叔丁基二甲基甲硅烷基）-甲氨蝶呤（N-4-N-（2,3-双叔丁基二甲基甲硅烷基氨基-6-蝶啶基甲基）-甲基氨基-苯甲酰谷氨酸-双（叔丁基二甲基甲硅烷基）酯）的效果取决于甲硅烷基化药物血脑屏障脂质溶解度和通透性的增加。
