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P-Glycoprotein, not BCRP, Limits the Brain Uptake of [(18)F]Mefway in Rodent Brain
Jae Yong Choi1, Jin Sook Song2, Minkyung Lee3
1Department of Nuclear Medicine, Gangnam Severance Hospital, Yonsei University College of Medicine, 712, Eonjuro, Gangnam-Gu, Seoul, 135-720, Korea.
Purpose:
The aim of this study was to determine whether the brain uptake of [(18)F]Mefway is influenced by the action of P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp) in rodents.
Procedures:
[(18)F]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:
[(18)F]Mefway is modulated by P-gp, and not by Bcrp in rodents.
