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Bioorg Med Chem. 2012 Jun 15;20(12):3703-9. doi: 10.1016/j.bmc.2012.04.051. Epub 2012 Apr 30.

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

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Molecular Imaging Medicinal Chemistry Laboratory, Riken Center for Molecular Imaging Science (CMIS), 6-7-3 Mintojima-minamimachi, Chuo-ku, Kobe, Hyogo, Japan.


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 [(11)C]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-[(11)C]methylation (viz., the rapid cross-coupling between [(11)C]methyl iodide and a boron intermediate).

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