First automatic radiosynthesis of 11C labeled Telmisartan using a multipurpose synthesizer for clinical research use
- نوع فایل : کتاب
- زبان : انگلیسی
- مؤلف : Hitoshi Iimori Yoshinobu Hashizume Masahiro Sasaki Yoshinobu Kajiwara Yuichi Sugimoto Yuichi Sugiyama Yasuyoshi Watanabe Michio Senda
- چاپ و سال / کشور: 2011
Description
Objective Telmisartan, a nonpeptide angiotensin II AT1 receptor antagonist, is an antihypertensive drug. Positron emission tomography (PET) imaging with [11C]Telmisartan is expected to provide information about the whole body pharmacokinetics of telmisartan as well as the transport function of hepatic OATP1B3. We developed a first automatic preparation system of [11C]Telmisartan to applicable clinical research using a new 11C and 18F multipurpose synthesizer. Methods Two milligrams of precursor (1) in 5 ll of 1 M KOH in 0.5 ml of dimethyl sulfoxide was reacted with [11C]CH3I for 5 min at 120C. The resultant solution was hydrolyzed with 1 M NaOH at 100C for 3 min. The neutralization was carried out with acetic acid, followed by purification with high-performance liquid chromatography. The desired radioactive fraction was collected and solvent was replaced by 10 ml saline containing 0.3 ml of EtOH and 0.5 ml of PEG400, and then passed through a sterile 0.22 lm filter (Millex-GV, Millipore) to a pyrogen-free vial as the final product. Results The yield of [11C]Telmisartan for clinical research use was 16.8 ± 2.9% EOB as decay corrected (n = 8, mean ± SD) in 32–36 min. The radiochemical purity of [11C]Telmisartan was[97%, and specific activity was higher than 86.3 MBq/nmol. Conclusions We succeeded in the first synthesis of [11C]Telmisartan for clinical research use by appropriate quality tests.
Ann Nucl Med (2011) 25:333–337 DOI 10.1007/s12149-011-0466-2 Received: 15 October 2010 / Accepted: 5 January 2011 / Published online: 28 January 2011
