ArticleJournal of medicinal chemistry2021
Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold.
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Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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14citing papers in PubMed
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14 citing papers in PubMed, 21 citations in OpenAlex.
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Authors and funding
33 authors at 6 institutions in 3 countries.
Jian RongDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.
Wakana MoriDepartment of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.
Xiaotian XiaDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.
Michael A SchafrothThe Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, SR107 10550 North Torrey Pines Road, La Jolla, California 92037, United States.ORCID 0000-0002-5864-6766
Chunyu ZhaoDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.
Richard S VanDepartment of Chemistry and Biochemistry, University of Oklahoma, Norman, Oklahoma 73019, United States.
Tomoteru YamasakiDepartment of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.
Jiahui ChenDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.
Zhiwei XiaoDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.
Achi HaiderDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.
Daisuke OgasawaraThe Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, SR107 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Atsuto HiraishiDepartment of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.
Tuo ShaoDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.
Yiding ZhangDepartment of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.
Zhen ChenDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.
Fuwen PangDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.
Kuan HuDepartment of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.ORCID 0000-0003-2448-2254
Lin XieDepartment of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.
Masayuki FujinagaDepartment of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.
Katsushi KumataDepartment of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.
Yuancheng GouChemshuttle Incorporation, 1699 Huishan Blvd., Wuxi, Jiangsu 214174, China.
Yang FangChemshuttle Incorporation, 1699 Huishan Blvd., Wuxi, Jiangsu 214174, China.
Shuyin GuChemshuttle Incorporation, 1699 Huishan Blvd., Wuxi, Jiangsu 214174, China.
Huiyi WeiCenter of Cyclotron and PET Radiopharmaceuticals, Department of Nuclear Medicine and PET/CT-MRI Center, The First Affiliated Hospital of Jinan University, Guangzhou 510630, China.
Liang BaoChemshuttle Incorporation, 1699 Huishan Blvd., Wuxi, Jiangsu 214174, China.
Hao XuCenter of Cyclotron and PET Radiopharmaceuticals, Department of Nuclear Medicine and PET/CT-MRI Center, The First Affiliated Hospital of Jinan University, Guangzhou 510630, China.
Thomas L CollierDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.
Yihan ShaoDepartment of Chemistry and Biochemistry, University of Oklahoma, Norman, Oklahoma 73019, United States.ORCID 0000-0001-9337-341X
Richard E CarsonDepartment of Radiology and Biomedical Imaging, Yale University School of Medicine, New Haven, Connecticut 06520, United States.
Benjamin F CravattThe Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, SR107 10550 North Torrey Pines Road, La Jolla, California 92037, United States.ORCID 0000-0001-5330-3492
Lu WangCenter of Cyclotron and PET Radiopharmaceuticals, Department of Nuclear Medicine and PET/CT-MRI Center, The First Affiliated Hospital of Jinan University, Guangzhou 510630, China.ORCID 0000-0002-8049-1991
Ming-Rong ZhangDepartment of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.ORCID 0000-0002-3001-9605
Steven H LiangDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology, Harvard Medical School, Boston, Massachusetts 02114, United States.ORCID 0000-0003-1413-6315
Harvard University · USNational Institutes for Quantum Science and Technology · JPFirst Affiliated Hospital of Jinan University · CNScripps Research Institute · USUniversity of Oklahoma · USYale University · US
Funding
CHEMOPROTEOMIC METHODS FOR SERINE HYDROLASE INHIBITOR DEVELOPMENTR01DA033760 · NIDA · SCRIPPS RESEARCH INSTITUTE, THE · PI CRAVATT, BENJAMIN F, SCAMPAVIA, LOUIS DANIEL · 2012 to 2021
$5.1MNew PET tracers for neuroimaging of FAAH in endocannabinoid signalingK01DA038000 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2014 to 2018
$927kNovel PET Tracers for Imaging Monoacylglycerol Lipase in Endocannabinoid SignalingR33DA043507 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2019 to 2021
$851kNovel PET Tracers for Imaging Monoacylglycerol Lipase in Endocannabinoid SignalingR21DA043507 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2017 to 2018
$425kNIDA NIH HHS K01 DA038000NIDA NIH HHS R01 DA033760NIDA NIH HHS R21 DA043507NIDA NIH HHS R33 DA043507
Abstract
Monoacylglycerol lipase (MAGL) is a 33 kDa serine protease primarily responsible for hydrolyzing 2-arachidonoylglycerol into the proinflammatory eicosanoid precursor arachidonic acid in the central nervous system. Inhibition of MAGL constitutes an attractive therapeutic concept for treating psychiatric disorders and neurodegenerative diseases. Herein, we present the design and synthesis of multiple reversible MAGL inhibitor candidates based on a piperazinyl azetidine scaffold. Compounds
Indexed as
Positron-Emission TomographyAnimalsAzetidinesBinding SitesDose-Response Relationship, DrugHaplorhiniLigandsModels, MolecularMolecular StructureMonoacylglycerol LipasesRadiopharmaceuticalsRatsStructure-Activity RelationshipAzetidinesLigandsMonoacylglycerol LipasesRadiopharmaceuticals
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