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In Vivo Evaluation of P-Glycoprotein Modulation of 8 PET Radioligands Used Clinically

¹ Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Tokyo, Japan; ² Brain Research Institute, Niigata University, Niigata, Japan; ³ Department of Pharmacology, Tohoku University Graduate School of Medicine, Sendai, Japan; and ⁴ Department of Pharmacy, Nuclear Medicine and PET Research, Free University Medical Center, Amsterdam, The Netherlands

View larger version (11K): [in this window] [in a new window]   FIGURE 1.  Chemical structures of radioligands investigated.

View larger version (13K): [in this window] [in a new window]   FIGURE 2.  Time course of effects of CsA on brain uptake of 11C-verapamil and brain-to-blood ratios. Data are mean ± SD (n = 5).

View larger version (10K): [in this window] [in a new window]   FIGURE 3.  Uptake of radiotracers in brain, heart, and muscle in the 2 assays for evaluating P-gp modulation. (A) Assay 1: effect of treatment with CsA on uptake of 11C-TMSX. (B) Assay 2: effect of treatment with cold TMSX on uptake of 11C-verapamil. Data are mean ± SD (n = 5–6). Student t test was performed for comparison with control data.