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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 ?-8 dependent transmembrane AMPA receptor regulatory protein by PET.

ABSTRACT: 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 ?-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 ?-8 dependent receptors in vivo.

SUBMITTER: Yu Q

PROVIDER: S-EPMC7045276 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature

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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.

Yu Qingzhen Q Kumata Katsushi K Li Hua H Zhang Yiding Y Chen Zhen Z Zhang Xiaofei X Shao Tuo T Hatori Akiko A Yamasaki Tomoteru T Xie Lin L Hu Kuan K Wang Gangqiang G Josephson Lee L Sun Shaofa S Zhang Ming-Rong MR Liang Steven H SH

Bioorganic & medicinal chemistry letters 20191217 4

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. ...[more]

PMID: 31879207

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