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

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


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).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP-Binding Cassette Transporters / analysis*
  • ATP-Binding Cassette Transporters / metabolism
  • Animals
  • Liver / chemistry*
  • Liver / metabolism
  • Liver-Specific Organic Anion Transporter 1
  • Male
  • Organic Anion Transporters / analysis*
  • Organic Anion Transporters / metabolism
  • Positron-Emission Tomography*
  • Pravastatin / analogs & derivatives*
  • Pravastatin / chemical synthesis
  • Pravastatin / chemistry
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Rats
  • Rats, Sprague-Dawley


  • ((11)C)dehydropravastatin
  • ATP-Binding Cassette Transporters
  • Abcc2 protein, rat
  • Liver-Specific Organic Anion Transporter 1
  • Organic Anion Transporters
  • Radiopharmaceuticals
  • SLCO1B1 protein, human
  • Pravastatin