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 language | English |
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Pages (from-to) | 267-273 |
Number of pages | 7 |
Journal | Molecular Imaging and Biology |
Volume | 18 |
Issue number | 2 |
DOIs | |
State | Published - 1 Apr 2016 |
Keywords
- Breast cancer resistance protein
- P-glycoprotein
- PET
- [F]Mefway