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11C-Loperamide is an avid substrate for P-glycoprotein (P-gp), but it is rapidly metabolized to 11C-N-desmethyl-loperamide (11C-dLop), which is also a substrate for P-gp and thereby contaminates the radioactive signal in the brain. Should further demethylation of 11C-dLop occur, radiometabolites with low entry into the brain are generated. Therefore, we evaluated the ability of 11C-dLop to quantify the function of P-gp at the blood-brain barrier in monkeys.

P-Glycoprotein Function at the Blood–Brain Barrier Imaged Using 11C-N-Desmethyl-Loperamide in Monkeys

P-Glycoprotein Function at the Blood–Brain Barrier Imaged Using ¹¹C-N-Desmethyl-Loperamide in Monkeys