Synthesis of [11C]dehydropravastatin, a PET probe potentially useful for studying OATP1B1 and MRP2 transporters in the liver

被引：23

作者：

Ijuin, Ryosuke ^{[1
]}

Takashima, Tadayuki ^{[2
]}

Watanabe, Yasuyoshi ^{[2
]}

Sugiyama, Yuichi ^{[3
]}

Suzuki, Masaaki ^{[1
]}

机构：

[1] RIKEN, Mol Imaging Med Chem Lab, Ctr Mol Imaging Sci, Chuo Ku, Kobe, Hyogo, Japan

[2] RIKEN, Mol Probe Dynam Lab, Ctr Mol Imaging Sci, Chuo Ku, Kobe, Hyogo, Japan

[3] Univ Tokyo, Grad Sch Pharmaceut Sci, Bunkyo Ku, Tokyo 1130033, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2012年 / 20卷 / 12期

关键词：

Positron emission tomography; C-C Coupling; Rapid reaction; Transporter; COA REDUCTASE INHIBITORS; PRAVASTATIN;

D O I：

10.1016/j.bmc.2012.04.051

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Drug transporters mediate the uptake and elimination of drugs in various organs; therefore, having knowledge of how a transporter functions in the body would play a key role in ensuring drug efficacy in in vivo systems. In this context, we designed and synthesized [C-11]dehydropravastatin, a novel PET probe that would be potentially useful for evaluation of the functions of the OATP1B1 and MRP2 transporters, based on the use of palladium(0)-mediated rapid C-[C-11]methylation (viz., the rapid cross-coupling between [C-11] methyl iodide and a boron intermediate). (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：3703 / 3709

页数：7

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