Roberts S, Bawdon R, Sobhi S, Dax J, Gilstrap L, Wimberly D
Department of Obstetrics and Gynecology, University of Texas Southwestern Medical Center.
Am J Obstet Gynecol. 1995 Jan;172(1 Pt 1):88-91. doi: 10.1016/0002-9378(95)90089-6.
The purpose of this study was to elucidate the maternal-fetal transfer of bisheteroypiperazine (U-87201-E), a nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus-1.
Placentas from normal term deliveries were used in this study to determine the maternal-fetal transfer of bisheteroypiperazine. The studies were conducted at several concentrations with the circulation either open-open or closed-closed.
In this study we determined that the clearance index of bisheteroypiperazine was 0.72 +/- 0.17 at maternal concentrations of 1.0 and 20.0 micrograms/ml. This is at least twice the clearance index of 3'-azido-2',3'-dideoxythymidine and more than five times greater than that of 2',3'-dideoxyinosine.
Bisheteroypiperazine crosses the maternal-fetal membranes by simple diffusion, in some instances almost equivalent to the reference compound antipyrine. Placental tissue concentrations were equivalent at all maternal concentrations, suggesting saturation. This high rate of maternal-fetal transfer suggests that it may be an effective prophylactic drug for fetuses of human immunodeficiency virus-infected mothers.
本研究旨在阐明双杂环哌嗪（U - 87201 - E），一种人类免疫缺陷病毒1型的非核苷类逆转录酶抑制剂的母婴转运情况。
本研究使用足月正常分娩的胎盘来确定双杂环哌嗪的母婴转运。研究在几种浓度下进行，循环模式为开放 - 开放或封闭 - 封闭。
在本研究中，我们确定在母体浓度为1.0和20.0微克/毫升时，双杂环哌嗪的清除指数为0.72±0.17。这至少是3'-叠氮-2'，3'-双脱氧胸苷清除指数的两倍，比2'，3'-双脱氧肌苷的清除指数高出五倍多。
双杂环哌嗪通过简单扩散穿过母胎膜，在某些情况下几乎等同于参考化合物安替比林。在所有母体浓度下，胎盘组织浓度均相等，表明存在饱和现象。这种高母婴转运率表明它可能是人类免疫缺陷病毒感染母亲胎儿的一种有效预防药物。
