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本实验建立了一个在氧化还原基础上的雌二醇(E_2)化学转运体系(E_2-CDS)。E_2与N-甲基烟酸的二氢吡啶衍生物以化学方式结合形成高度脂溶性的E_2-CDS,很容易通过血脑屏障,在脑内被氧化成E_2季氨毗啶盐(E_2-Quat),亲水性强,不易通过血脑屏障,要在脑内去掉载体,才能将E_2释放出来。E_2-CDS的这一特性使正常情况下不能通过血脑屏障的E_2能够持久地从脑内释放到外周,避免给予E_2所引起的外周类固醇反应,延长给药间隔,减少给药量,使雌激素的使用更加广泛安全。
In this experiment, a redox-based estradiol (E 2) chemical transport system (E 2 -CDS) was established. E_2 and dihydropyridine derivatives of N-methylnicotinic acid chemically combine to form highly lipophilic E 2 -CDS, which easily passes through the blood-brain barrier and is oxidized to E 2 quaternary ammonium salt (E 2 -Quat ), Hydrophilic, difficult to pass the blood-brain barrier, to remove the vector in the brain, in order to release E_2. This characteristic of E_2-CDS enables E_2, which normally can not cross the blood-brain barrier, to be released from the brain to the periphery permanently, avoiding the peripheral steroid response caused by E_2, prolonging the interval between administrations and decreasing the dosage, The use of hormones is more extensive and safe.