153750-28-8Relevant articles and documents
Evaluation of [18F]pitavastatin as a positron emission tomography tracer for in vivo organic transporter polypeptide function
Yagi, Yusuke,Kimura, Hiroyuki,Okuda, Haruka,Ono, Masahiro,Nakamoto, Yuji,Togashi, Kaori,Saji, Hideo
, p. 25 - 31 (2019)
Introduction: To understand the pathways involved in drug clearance from the body, quantitative evaluations of the hepatobiliary transport of drugs are important. The organic anion transporting polypeptide (OATP) family transporter, particularly OATP1B1 and 1B3, are considered to play an important role in hepatic uptake of organic anion compounds. Pitavastatin is a substrate of OATP, and it includes a fluorine group. Therefore, it represents an acceptable positron-emission tomography (PET) tracer using fluorine-18 to image in vivo hepatic transporter functions. Method: [18F]Pitavastatin was synthesized using the method we previously reported. To evaluate the potential of [18F]pitavastatin in PET imaging of in vivo OATP functions, we investigated the hepatic uptake with/without rifampicin as an OATP inhibitor after administration in normal SD rats. [18F]Pitavastatin metabolite was evaluated using reverse-phase thin-layer chromatography (TLC) autoradiography. We subsequently analyzed the PET image results and demonstrated that [18F]pitavastatin selectively accumulated in the liver post-administration. Result and discussion In metabolite analysis using reverse-phase TLC, we found that the radioactivity detected in the plasma, liver (>90% intact), and bile mostly originated from the parent pitavastatin of the PET study (~40 min). [18F]pitavastatin's hepatic uptake decreased (approximately 76%) with rifampicin co-administration in PET analysis. Because [18F]pitavastatin has lower clearance in rats than other previously reported OATP1B PET s, it holds the potential of an imaging tracer that has a higher sensitivity in monitoring hepatic OATP1B function's changes. Conclusion: Compared with the previously reported OATP imaging tracers, [18F]pitavastatin is more suitable for the sensitive detection of functional changes in OATP transporters. We believe that [18F]pitavastatin enables quantitative analysis of the hepatobiliary transport system for organic anion compounds.
No-carrier added synthesis of 18F-labelled nucleosides using Stille cross-coupling reactions with 4-[18F]fluoroiodobenzene
Wuest, Frank R.,Kniess, Torsten
, p. 457 - 468 (2004)
The radiosyntheses of 5-(4′-[18F]fluorophenyl)-uridine [18F]-11 and 5-(4′-[18F]fluorophenyl)-2′- deoxy-uridine [18F]-12 are described. The 5-(4′-[ 18F]fluoro-phenyl)-substituted nucleosides were prepared via a Stille cross-coupling reaction with 4-[18F]fluoroiodobenzene followed by basic hydrolysis using 1M potassium hydroxide. The Stille cross-coupling reaction was optimized by screening various palladium complexes, additives and solvents. By using optimized labelling conditions (Pd2(dba) 3/CuI/AsPh3 in DMF/dioxane (1:1), 20min at 65°C), 550MBq of [4-18F]fluoroiodobenzene could be converted into 120MBq (33%, decay-corrected) of 5-(4′-[18F]fluorophenyl)-2′- deoxy-uridine [18F]-12 within 40min, including HPLC purification.
Development of a novel [18F]fluorobenzyl derivative of the AT1 receptor antagonist Candesartan
Alonso Martinez, Luis Michel,DaSilva, Jean N.
, p. 120 - 128 (2020/11/30)
Candesartan is a clinically approved angiotensin II type 1 receptor (AT1R)-blocker that selectively binds AT1Rs in high affinity. We report here the radiosynthesis and automation of the novel [18F]fluorobenzyl derivative o
COPPER CATALYZED [18F]FLUORINATION OF IODONIUM SALTS
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Paragraph 0064; 0066; 0079, (2017/04/28)
Copper-catalyzed radiofluorination of iodonium salts, iodonium salts, and compounds obtained by copper-catalyzed radiofluorination of iodonium salts are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.
