Document 0271
 DOCN  M9550271
 TI    The maternal-fetal transfer of bisheteroypiperazine (U-87201-E) in the
       ex vivo human placenta.
 DT    9505
 AU    Roberts S; Bawdon R; Sobhi S; Dax J; Gilstrap L 3rd; Wimberly D;
       Department of Obstetrics and Gynecology, University of Texas;
       Southwestern Medical Center.
 SO    Am J Obstet Gynecol. 1995 Jan;172(1 Pt 1):88-91. Unique Identifier :
       AIDSLINE MED/95150224
 AB    OBJECTIVE: 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. 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 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. CONCLUSIONS:
       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.
 DE    Female  Fetal Blood/METABOLISM  Human  *Maternal-Fetal Exchange  Osmolar
       Concentration  Piperazines/*PHARMACOKINETICS  Placenta/*METABOLISM
       Pregnancy  Reverse Transcriptase/ANTAGONISTS & INHIB  Support, Non-U.S.
       Gov't  JOURNAL ARTICLE

       SOURCE: National Library of Medicine.  NOTICE: This material may be
       protected by Copyright Law (Title 17, U.S.Code).