title: Synthesis of [(11)C]dehydropravastatin, a PET probe potentially useful for studying OATP1B1 and MRP2 transporters in the liver.
abstract: 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).
authors.affiliation: Molecular Imaging Medicinal Chemistry Laboratory, Riken Center for Molecular Imaging Science (CMIS), 6-7-3 Mintojima-minamimachi, Chuo-ku, Kobe, Hyogo, Japan.
authors.forename: Ryosuke
authors.initials: R
authors.lastname: Ijuin
authors.forename: Tadayuki
authors.initials: T
authors.lastname: Takashima
authors.forename: Yasuyoshi
authors.initials: Y
authors.lastname: Watanabe
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Sugiyama
authors.forename: Masaaki
authors.initials: M
authors.lastname: Suzuki
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000032:analysis* / Q000378:metabolism; D000818:Animals; D008099:Liver / Q000737:chemistry* / Q000378:metabolism; D027381:Liver-Specific Organic Anion Transporter 1; D008297:Male; D027361:Organic Anion Transporters / Q000032:analysis* / Q000378:metabolism; D049268:Positron-Emission Tomography; D017035:Pravastatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: C576515:((11)C)dehydropravastatin; D018528:ATP-Binding Cassette Transporters; C423013:Abcc2 protein, rat; D027381:Liver-Specific Organic Anion Transporter 1; D027361:Organic Anion Transporters; D019275:Radiopharmaceuticals; C503999:SLCO1B1 protein, human; D017035:Pravastatin