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Publication : P-Glycoprotein, not BCRP, Limits the Brain Uptake of [(18)F]Mefway in Rodent Brain.

First Author  Choi JY Year  2016
Journal  Mol Imaging Biol Volume  18
Issue  2 Pages  267-73
PubMed ID  26250653 Mgi Jnum  J:329794
Mgi Id  MGI:6869131 Doi  10.1007/s11307-015-0883-z
Citation  Choi JY, et al. (2016) P-Glycoprotein, not BCRP, Limits the Brain Uptake of [(18)F]Mefway in Rodent Brain. Mol Imaging Biol 18(2):267-73
abstractText  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.
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