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Evaluation of In Vivo P-Glycoprotein Function at the Blood–Brain Barrier Among MDR1 Gene Polymorphisms by Using 11 C-Verapamil

By Akihiro Takano, Hiroyuki Kusuhara, Tetsuya Suhara, Ichiro Ieiri, Takuya Morimoto, Young-joo Lee, Jun Maeda, Yoko Ikoma, Hiroshi Ito, Kazutoshi Suzuki and Yuichi Sugiyama


P-glycoprotein (P-gp) is a membrane protein that functions as an adenosine triphosphate–dependent efflux pump for xenobiotics at the blood–brain barrier (BBB). Polymorphisms of MDR1 gene have been reported to be associated with the expression level of P-gp. 11C-Verapamil is considered to be one of the suitable radioligands for evaluating P-gp functions. However, the metabolites of verapamil might complicate the quantitative analysis because of their possible brain penetration. In the present study, we investigated the P-gp functional differences at the BBB between the haplotypes (1236TT, 2677TT, 3435TT vs. 1236CC, 2677GG, 3435CC) of the MDR1 gene with different quantitative analyses of 11C-verapamil. Methods: Thirty-three healthy male volunteers were enrolled in this study after identification of the haplotypes of the MDR1 gene. Brain PET scans with 11C-verapamil were performed for 16 min. Integration plot analysis, which yields brai

Year: 2013
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