核化学与放射化学2011，Vol.33Issue(3)：188-192,5.
Aβ斑块显像剂：11C-PIB的合成及标记
Synthesis and Carbon Labeling of 11C-PIB for Aβ-Amyloid Imaging
摘要
Abstract
Assessing the deposition of Aβ-amyloid in the living brain is important for diagno-sis and treatment of Alzheimer' s disease (AD). 2-( 4'-N-11C-methyl-aminophenyl )-6-hydroxybenzothiazole(11 C-PIB) was used as a ideal labeled probe imaging Aβ-amyloid for AD. The precursor of 11C-PIB, 2-(4'-aminophenyl)-6-hydroxybenzothiazole, was synthe-sized. 11-PIB was labeled with 11C-CH3-Triflate(Trifluoromethanesulfonate) under unpro-tect 6-hydroxyl precursor at room temperature. The labeling yield, radiochemistry purity and specific activity are 52.6%(corrected, n = 35), 99% and 18. 0 TBq/mmoL respectively. The by-reaction occurrs when the reaction is heated 80 ℃ for 2 min. The radiochemistry purity can be improved to 99% by semi-HPLC weak acid mobile phase.关键词
Aβ斑块显像剂；阿尔茨海默病(AD)；11C-PIBKey words
Aβ-amyloid imaging agent / AD/ 11C-PIB分类
医药卫生引用本文复制引用
张锦明,王武尚,张晓军,郭喆,田嘉禾..Aβ斑块显像剂：11C-PIB的合成及标记[J].核化学与放射化学,2011,33(3):188-192,5.基金项目
国家自然科学基金资助项目(30670586)；核能开发科技资助项目(2009-1228) （30670586）
