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In this study, we assessed the effect of thiethylperazine, an antiemetic drug which was shown to stimulate MRP1 activity in vitro and to decrease A\u03b2 load in a rapid \u03b2-amyloidosis mouse model (APP\/PS1-21), on MRP1 transport activity by means of positron emission tomography (PET) imaging with the MRP1 tracer 6-bromo-7-[11C]methylpurine. Groups of wild-type, APP\/PS1-21 and Abcc1(\u2212\/\u2212) mice underwent PET scans before and after a 5-day oral treatment period with thiethylperazine (15 mg\/kg, once daily). The elimination rate constant of radioactivity (kelim) was calculated from time\u2013activity curves in the brain and the lungs as a measure of tissue MRP1 activity. Treatment with thiethylperazine had no significant effect on MRP1 activity in the brain and the lungs of wild-type and APP\/PS1-21 mice. 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