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

Title
P-Glycoprotein, not BCRP, Limits the Brain Uptake of [F-18]Mefway in Rodent Brain
Authors
Choi, Jae YongSong, Jin SookLee, MinkyungCho, Woon-KiChung, JinLyoo, Chul HyoungKim, Chul HoonPark, JiaeLee, Kyo ChulKim, Kyeong MinKang, Jee HaeBae, Myung AeRyu, Young Hoon
Ewha Authors
정진
SCOPUS Author ID
정진scopus
Issue Date
2016
Journal Title
MOLECULAR IMAGING AND BIOLOGY
ISSN
1536-1632JCR Link

1860-2002JCR Link
Citation
MOLECULAR IMAGING AND BIOLOGY vol. 18, no. 2, pp. 267 - 273
Keywords
[F-18] MefwayP-glycoproteinBreast cancer resistance proteinPET
Publisher
SPRINGER
Indexed
SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
Purpose The aim of this study was to determine whether the brain uptake of [F-18]Mefway is influenced by the action of P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp) in rodents. Procedures: [F-18]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: [F-18]Mefway is modulated by P-gp, and not by Bcrp in rodents.
DOI
10.1007/s11307-015-0883-z
Appears in Collections:
의과대학 > 의학과 > Journal papers
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