Hetero-aryl bromide precursor fluorine-18 radiosynthesis and preclinical evaluation of a novel positron emission tomography (PET) tracer [18F]GSK1482160.
Hetero-aryl bromide precursor fluorine-18 radiosynthesis and preclinical evaluation of a novel positron emission tomography (PET) tracer [18F]GSK1482160.
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DOI：
10.1016/j.bmc.2022.116996
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发表时间：
2022-09
影响因子：
3.5
通讯作者：
Guolong Huang;Xiaolei Lu;Yifan Qiu;Lei Bi;Peizhen Ye;Min Yang;Yanfang Shen;Hongjun Jin;Junbin Han
中科院分区：
文献类型：
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作者：
Guolong Huang;Xiaolei Lu;Yifan Qiu;Lei Bi;Peizhen Ye;Min Yang;Yanfang Shen;Hongjun Jin;Junbin Han
The purinergic P2X7 receptor (P2X7R), an ATP gated ion channel, is an important therapeutic target for various inflammatory immune and neurodegenerative diseases. A novel P2X7R targeting radiotracer GSK1482160 was radiosynthesized by hetero-aryl bromides precursor10with [18F]Et4NF, 20–30 % radiochemical yield, > 68 GBq/μmol specific activity, >98 % radiochemical purity. Evaluation in healthy male Sprague-Dawley rats revealed that [18F]GSK1482160([18F]11)was stably retained 87.81 %, 72.45 %, and 56.32 % in brain, blood and liver respectively 60-min post-injection.Ex-vivobiodistribution of[18F]11proved that it was able to target the P2X7Rin vivoand there was no defluorination in the major organs. PET/MRI imaging and autoradiography revealed that[18F]11was able to penetrate the blood–brain barrier (BBB) and to be a promising P2X7R PET radioligand for clinical translation.
