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Design, Synthesis, and Evaluation of 18F-Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes.
Chen, Zhen; Mori, Wakana; Fu, Hualong; Schafroth, Michael A; Hatori, Akiko; Shao, Tuo; Zhang, Genwei; Van, Richard S; Zhang, Yiding; Hu, Kuan; Fujinaga, Masayuki; Wang, Lu; Belov, Vasily; Ogasawara, Daisuke; Giffenig, Pilar; Deng, Xiaoyun; Rong, Jian; Yu, Qingzhen; Zhang, Xiaofei; Papisov, Mikhail I; Shao, Yihan; Collier, Thomas L; Ma, Jun-An; Cravatt, Benjamin F; Josephson, Lee; Zhang, Ming-Rong; Liang, Steven H.
Afiliação
  • Chen Z; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Mori W; Department of Chemistry, School of Science , Tianjin University , 92 Weijin Road, Nankai District , Tianjin 300072 , China.
  • Fu H; Department of Radiopharmaceuticals Development , National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
  • Schafroth MA; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Hatori A; The 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.
  • Shao T; Department of Radiopharmaceuticals Development , National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
  • Zhang G; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Van RS; Department of Chemistry and Biochemistry , University of Oklahoma , Norman , Oklahoma 73019 , United States.
  • Zhang Y; Department of Chemistry and Biochemistry , University of Oklahoma , Norman , Oklahoma 73019 , United States.
  • Hu K; Department of Radiopharmaceuticals Development , National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
  • Fujinaga M; Department of Radiopharmaceuticals Development , National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
  • Wang L; Department of Radiopharmaceuticals Development , National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
  • Belov V; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Ogasawara D; Department of Nuclear Medicine and PET/CT-MRI Centre, the First Affiliated Hospital of Jinan University & Institute of Molecular and Functional Imaging , Jinan University , Guangzhou 510630 , China.
  • Giffenig P; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Deng X; Department of Research , Shriners Hospitals for Children , Boston , Massachusetts 02114 , United States.
  • Rong J; The 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.
  • Yu Q; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Zhang X; Department of Research , Shriners Hospitals for Children , Boston , Massachusetts 02114 , United States.
  • Papisov MI; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Shao Y; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Collier TL; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Ma JA; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Cravatt BF; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
  • Josephson L; Department of Research , Shriners Hospitals for Children , Boston , Massachusetts 02114 , United States.
  • Zhang MR; Department of Chemistry and Biochemistry , University of Oklahoma , Norman , Oklahoma 73019 , United States.
  • Liang SH; Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital, and Department of Radiology, Harvard Medical School , Boston , Massachusetts 02114 , United States.
J Med Chem ; 62(19): 8866-8872, 2019 10 10.
Article em En | MEDLINE | ID: mdl-31518130
ABSTRACT
Dysfunction of monoacylglycerol lipase (MAGL) is associated with several psychopathological disorders, including drug addiction and neurodegenerative diseases. Herein we design, synthesize, and evaluate several irreversible fluorine-containing MAGL inhibitors for positron emission tomography (PET) ligand development. Compound 6 (identified from a therapeutic agent) was advanced for 18F-labeling via a novel spirocyclic iodonium ylide (SCIDY) strategy, which demonstrated high brain permeability and excellent specific binding. This work supports further development of novel 18F-labeled MAGL PET probes.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Meios de Contraste / Inibidores Enzimáticos / Monoacilglicerol Lipases Limite: Animals Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Meios de Contraste / Inibidores Enzimáticos / Monoacilglicerol Lipases Limite: Animals Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Estados Unidos