Stephens M C, Bernatsky A, Singh H, Kanfer J N, Legler G
Biochim Biophys Acta. 1981 Jan 7;672(1):29-32. doi: 10.1016/0304-4165(81)90276-2.
The time course of the distribution of the beta-glucosidase inhibitor [3H]conduritol B epoxide was determined in various organs of mice, which had received a single interperitoneal dose of the inhibitor. The epoxide is rapidly distributed over all tissues except brain where its concentration is only one-tenth of the average. This is considered an indication that the epoxide can pass the blood/brain barrier only with difficulty. A 4-fold enrichment is seen in the kidney. The inhibitor is excreted with a half-life of about 7 h; it is not metabolized. A parallel determination of beta-glucosidase activity in the tissues showed greater than 90% inhibition within 1 and 2 h and a beginning recovery between 4 and 12 h. The only exception was brain, where no effects could be seen after 1 h and where a subsequent decrease to 37% of normal was observed after 12 h.
测定了单次腹腔注射β-葡萄糖苷酶抑制剂[3H]千金二萜醇环氧化物后，其在小鼠各器官中的分布时间进程。该环氧化物能迅速分布到除脑以外的所有组织中，脑内的浓度仅为平均浓度的十分之一。这被认为表明该环氧化物很难通过血脑屏障。在肾脏中观察到了4倍的富集。该抑制剂以约7小时的半衰期排泄；它不被代谢。对组织中β-葡萄糖苷酶活性的平行测定表明，在1至2小时内抑制率大于90%，在4至12小时之间开始恢复。唯一的例外是脑，在1小时后未观察到影响，而在12小时后观察到随后降至正常水平的37%。
