TY - JOUR
T1 - The maternal-fetal transfer of bisheteroypiperazine (U-87201-E) in the ex vivo human placenta
AU - Roberts, Scott
AU - Bawdon, Robert
AU - Sobhi, Sorab
AU - Dax, Jody
AU - Gilstrap, Larry
AU - Wimberly, David
PY - 1995/1
Y1 - 1995/1
N2 - OBJECTIVE: The purpose of this study was to elucidate the maternal-fetal transfer of bisheteroypiperazine (U-87201-E), a nonnucleoside reverse transcriptasae inhibitor of human immunodeficiency virus-1. STUDY DESIGN: 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. RESULTS: 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 μg/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. CONCLUSIONS: Bisheteroypiperazine crosses the maternal-fetal membranes by simple diffusion, in some instances almost equivalent to the refernece 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.
AB - OBJECTIVE: The purpose of this study was to elucidate the maternal-fetal transfer of bisheteroypiperazine (U-87201-E), a nonnucleoside reverse transcriptasae inhibitor of human immunodeficiency virus-1. STUDY DESIGN: 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. RESULTS: 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 μg/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. CONCLUSIONS: Bisheteroypiperazine crosses the maternal-fetal membranes by simple diffusion, in some instances almost equivalent to the refernece 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.
KW - Bisheteroypiperazine
KW - ex vivo human placenta
KW - rapid simple diffusion
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U2 - 10.1016/0002-9378(95)90089-6
DO - 10.1016/0002-9378(95)90089-6
M3 - Article
C2 - 7531400
AN - SCOPUS:0028919141
SN - 0002-9378
VL - 172
SP - 88
EP - 91
JO - American journal of obstetrics and gynecology
JF - American journal of obstetrics and gynecology
IS - 1 PART 1
ER -