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10-[11C]methoxy-20(S)-camptothecin
APPLIED RADIATION AND ISOTOPES · 2012 · IF 1.172

Simple automated radiosynthesis of 10-[11C]methoxy-20(S)-camptothecin and biodistribution in normal mice

Zhen-feng Liu,Guo-lin Wang,Meng-jie Dong,Qian Zhang,Jia-jun Li,Kui Zhao,Shu-ye Yang,Xiang-tong Lin

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.

CAS / MDL: 64439-81-2
研究领域: 药理学 · 核医学 · 肿瘤学
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