Effects of Selected OATP and/or ABC Transporter Inhibitors on the Brain and Whole-Body Distribution of Glyburide
作者: Nicolas TournierWadad SabaSalvatore CisterninoMarie-Anne PeyronneauAnnelaure DamontSébastien GoutalAlbertine DuboisFrédéric DolléJean-Michel ScherrmannHéric ValetteBertrand KuhnastMichel Bottlaender
作者单位: 1CEA, DSV, I2BM, Service Hospitalier Frédéric Joliot
2INSERM U705, CNRS UMR8206, Faculté de Pharmacie, Université Paris Descartes, Sorbonne Paris Cité, Université Paris Diderot
3Assistance Publique–Hôpitaux de Paris
刊名: The AAPS Journal, 2013, Vol.15 (4), pp.1082-1090
来源数据库: Springer Journal
DOI: 10.1208/s12248-013-9514-2
关键词: ABC transportersblood–brain barrierglyburideorganic anion transporting polypeptidepositron emission tomography
英文摘要: Abstract(#br)Glyburide (glibenclamide, GLB) is a widely prescribed antidiabetic with potential beneficial effects in central nervous system injury and diseases. In vitro studies show that GLB is a substrate of organic anion transporting polypeptide (OATP) and ATP-binding cassette (ABC) transporter families, which may influence GLB distribution and pharmacokinetics in vivo . In the present study, we used [ 11 C]GLB positron emission tomography (PET) imaging to non-invasively observe the distribution of GLB at a non-saturating tracer dose in baboons. The role of OATP and P-glycoprotein (P-gp) in [ 11 C]GLB whole-body distribution, plasma kinetics, and metabolism was assessed using the OATP inhibitor rifampicin and the dual OATP/P-gp inhibitor cyclosporine. Finally, we used in situ brain...
全文获取路径: Springer  (合作)
影响因子:4.386 (2012)

  • ABC ABC automatic coding system