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1篇 您的检索式：作者名="Thomas L.Collier"

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		题名	作者	年代	出处	被引量
	1	Development of a highly-specific ^(18)F-labeled irreversible positron emission tomography tracer for monoacylglycerol lipase mapping显示文摘As a serine hydrolase,monoacylglycerol lipase(MAGL) is principally responsible for the metabolism of 2-arachidonoylglycerol(2-AG) in the central nervous system(CNS),leading to the formation of arachidonic acid(AA).Dysfunction of MAGL has been associated with multiple CNS disorders and symptoms,including neuroinflammation,cognitive impairment,epileptogenesis,nociception and neurodegenerative diseases.Inhibition of MAGL provides a promising therapeutic direction for the treatment of these conditions,and a MAGL positron emission tomography(PET) probe would greatly facilitate preclinical and clinical development of MAGL inhibitors.Herein,we design and synthesize a small library of fluoropyridyl-containing MAGL inhibitor candidates.Pharmacological evaluation of these candidates by activity-based protein profiling identified 14 as a lead compound,which was then radiolabeled with fluorine-18 via a facile SNAr reaction to form 2-[^(18)F]fluoropyridine scaffold.Good blood-brain barrier permeability and high in vivo specific binding was demonstrated for radioligand [^(18)F]14(also named as [^(18)F]MAGL-1902).This work may serve as a roadmap for clinical translation and further design of potent 18F-labeled MAGL PET tracers.	Zhen Chen Wakana Mori Jian Rong Michael A.Schafroth Tuo Shao Richard S.Van Daisuke Ogasawara Tomoteru Yamasaki Atsuto Hiraishi Akiko Hatori Jiahui Chen Yiding Zhang Kuan Hu Masayuki Fujinaga Jiyun Sun Qingzhen Yu Thomas L.Collier Yihan Shao Benjamin F.Cravatt Lee Josephson Ming-Rong Zhang Steven H.Liang	2021	Acta Pharmaceutica Sinica B2021，11，6：	0

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