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Synthesis and evaluation of 6-(11C-methyl(4-(pyridin-2-yl)thiazol-2-yl)amino)benzo[d]thiazol-2(3H)-one for imaging γ-8 dependent transmembrane AMPA receptor regulatory protein by PET.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-12-17 , DOI: 10.1016/j.bmcl.2019.126879
Qingzhen Yu 1 , Katsushi Kumata 2 , Hua Li 1 , Yiding Zhang 2 , Zhen Chen 1 , Xiaofei Zhang 1 , Tuo Shao 1 , Akiko Hatori 2 , Tomoteru Yamasaki 2 , Lin Xie 2 , Kuan Hu 2 , Gangqiang Wang 3 , Lee Josephson 1 , Shaofa Sun 3 , Ming-Rong Zhang 2 , Steven H Liang 1
Affiliation  

Transmembrane AMPA receptor regulatory proteins (TARPs) are a recently discovered family of proteins that modulate AMPA receptors activity. Based on a potent and selective TARP subtype γ-8 antagonist, 6-(methyl(4-(pyridin-2-yl)thiazol-2-yl)amino)benzo[d]thiazol-2(3H)-one (compound 9), we perform the radiosynthesis of its 11C-isotopologue 1 and conduct preliminary PET evaluation to test the feasibility of imaging TARP γ-8 dependent receptors in vivo.

中文翻译:

合成和评估6-(11C-甲基(4-(吡啶-2-基)噻唑-2-基)氨基)苯并[d]噻唑-2(3H)-用于成像依赖于γ-8的跨膜AMPA受体调节剂蛋白质由PET制成。

跨膜AMPA受体调节蛋白(TARP)是最近发现的可调节AMPA受体活性的蛋白家族。基于强效且选择性的TARP亚型γ-8拮抗剂,6-(甲基(4-(吡啶-2-基)噻唑-2-基)氨基)苯并[d]噻唑-2(3H)-(化合物9 ),我们进行了11C-同位素异构体1的放射性合成,并进行了初步的PET评估,以测试在体内成像TARPγ-8依赖性受体的可行性。
更新日期:2019-12-18
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