P-Glycoprotein, not BCRP, Limits the Brain Uptake of [18F]Mefway in Rodent Brain

Jae Yong Choi, Jin Sook Song, Minkyung Lee, Woon Ki Cho, Jin Chung, Chulhyoung Lyoo, Chul Hoon Kim, Jiae Park, Kyo Chul Lee, Kyeong Min Kim, Jee Hae Kang, Myung Ae Bae, Young Hoon Ryu

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Abstract

Purpose: The aim of this study was to determine whether the brain uptake of [18F]Mefway is influenced by the action of P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp) in rodents. Procedures: [18F]Mefway was applied to rats pharmacologically inhibited with tariquidar (TQD) and to genetically disrupted mice. Results: Pretreatment of TQD results in 160 % higher hippocampal uptake compared with control rats. In genetically disrupted mice, a maximal brain uptake value of 3.2 SUV in the triple knockout mice (tKO, Mdr1a/b(−/−)Bcrp1(−/−)) was comparable to that of the double knockout mice (dKO, Mdr1a/b(−/−)) and 2-fold those of the wild-type and Bcrp1(−/−) knockout mice. The differences of binding values were statistically insignificant between control and experimental groups. The brain-to-plasma ratios for tKO mice were also two to five times higher than those for other groups. Conclusions: [18F]Mefway is modulated by P-gp, and not by Bcrp in rodents.

Original languageEnglish
Pages (from-to)267-273
Number of pages7
JournalMolecular Imaging and Biology
Volume18
Issue number2
DOIs
Publication statusPublished - 2016 Apr 1

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All Science Journal Classification (ASJC) codes

  • Oncology
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

Cite this

Choi, J. Y., Song, J. S., Lee, M., Cho, W. K., Chung, J., Lyoo, C., Kim, C. H., Park, J., Lee, K. C., Kim, K. M., Kang, J. H., Bae, M. A., & Ryu, Y. H. (2016). P-Glycoprotein, not BCRP, Limits the Brain Uptake of [18F]Mefway in Rodent Brain. Molecular Imaging and Biology, 18(2), 267-273. https://doi.org/10.1007/s11307-015-0883-z