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Synthesis and evaluation of [11C]XR9576 to assess the function of drug efflux transporters using PET

✍ Scribed by Kazunori Kawamura; Fujiko Konno; Joji Yui; Tomoteru Yamasaki; Akiko Hatori; Kazuhiko Yanamoto; Hidekatsu Wakizaka; Makoto Takei; Nobuki Nengaki; Toshimitsu Fukumura; Ming-Rong Zhang

Book ID
107615324
Publisher
Springer Japan
Year
2010
Tongue
English
Weight
268 KB
Volume
24
Category
Article
ISSN
0914-7187

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The utility of the diaminoquinazoline derivative CP-100,356 as an in vivo probe to selectively assess MDR1/BCRP-mediated drug efflux was examined in the rat. CP-100,356 was devoid of inhibition (IC 50 >50 mM) against major human P450 enzymes including P4503A4. In human MDR1-transfected MDCKII cells,