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

Qingzhen Yu,Katsushi Kumata,Hua Li,Yiding Zhang,Zhen Chen,Xiaofei Zhang,Tuo Shao,Akiko Hatori,Tomoteru Yamasaki,Lin Xie,Kuan Hu,Gangqiang Wang,Lee Josephson,Shaofa Sun,Ming-Rong Zhang,Steven H Liang

doi:10.1016/j.bmcl.2019.126879

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

Qingzhen Yu, Katsushi Kumata + Show 14 more

Open Access

https://doi.org/10.1016/j.bmcl.2019.126879

Copy DOI

Journal: Bioorganic & Medicinal Chemistry Letters	Publication Date: Dec 17, 2019
Citations: 2

Affiliation: Massachusetts General Hospital, National Institutes for Quantum and Radiological Science and Technology, Hubei University of Science and Technology

#Transmembrane AMPA Receptor Regulatory Proteins #AMPA Receptor + Show 8 more

Abstract
Full-Text PDF
Similar Papers

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 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.

Full Text