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.
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.
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6-(11C-甲基(4-(吡啶-2-基)噻唑-2-基)氨基)苯并[d]噻唑-2(3H)-一的合成和评估用于成像γ-8依赖性跨膜AMPA受体调节
DOI：
10.1016/j.bmcl.2019.126879
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发表时间：
2020
影响因子：
2.7
通讯作者：
Liang,StevenH
中科院分区：
文献类型：
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作者：
Yu,Qingzhen;Kumata,Katsushi;Li,Hua;Zhang,Yiding;Chen,Zhen;Zhang,Xiaofei;Shao,Tuo;Hatori,Akiko;Yamasaki,Tomoteru;Xie,Lin;Hu,Kuan;Wang,Gangqiang;Josephson,Lee;Sun,Shaofa;Zhang,Ming-Rong;Liang,StevenH
跨膜AMPA受体调节蛋白(TARP)是新近发现的调节AMPA受体活性的蛋白质家族。基于一种有效和选择性的TARP亚型6-(methyl(4-(pyridin-2-yl)thiazol-2-yl)amino)benzo[d]thiazol-2(3H)-one-8拮抗剂γ(化合物9)，我们进行了其11C-同位素的放射合成，并进行了初步的正电子发射计算机断层扫描，以测试体内成像TARPγ-8依赖的受体的可行性。
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 (compound9), we perform the radiosynthesis of its11C-isotopologue1and conduct preliminary PET evaluation to test the feasibility of imaging TARP γ-8 dependent receptorsin vivo.