title: Simple automated radiosynthesis of 10-[11C]methoxy-20(S)-camptothecin and biodistribution in normal mice.
abstract: 10-[(11)C]methoxy-20(S)-camptothecin was synthesized automatically. The radiochemical yield was 30%-50% (all calculated at EOB, n=20) with [(11)C]methyl triflate as a methylating agent. The radiochemical purity was greater than 96%, and the specific activity was 8.72±2.18 GBq/μmoL at EOS. Biodistribution showed that 10-[(11)C]methoxy-20(S)-camptothecin is characterized by quick clearance from the blood and by significant uptake in the liver (5.72±1.92% ID/g at 15 min), intestines (2.43±0.38% ID/g at 15 min), and kidney (1.57±0.85% ID/g at 15 min). Micro-PET imaging clearly showed high radioactivity accumulation in liver, intestines and bladder, indicating that the primary modes of excretion of the radiotracer are through the hepatobiliary system and, to a lesser extent, through the renal system.
authors.affiliation: PET Center, The First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou 310003, China.
authors.forename: Zhen-feng
authors.initials: ZF
authors.lastname: Liu
authors.forename: Guo-lin
authors.initials: GL
authors.lastname: Wang
authors.forename: Meng-jie
authors.initials: MJ
authors.lastname: Dong
authors.forename: Qian
authors.initials: Q
authors.lastname: Zhang
authors.forename: Jia-jun
authors.initials: JJ
authors.lastname: Li
authors.forename: Kui
authors.initials: K
authors.lastname: Zhao
authors.forename: Shu-ye
authors.initials: SY
authors.lastname: Yang
authors.forename: Xiang-tong
authors.initials: XT
authors.lastname: Lin
mesh_terms: D000818:Animals; D001331:Automation; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D007413:Intestinal Mucosa / Q000378:metabolism; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D051379:Mice; D008813:Mice, Inbred ICR; D049268:Positron-Emission Tomography / Q000379:methods; D014018:Tissue Distribution
chemical_list: C577311:10-methoxycamptothecin; D002166:Camptothecin