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Synthesis and preclinical evaluation of 11C-labeled 7-Oxo-2,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridine radioligands for RIPK1 positron emission tomography imaging

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机构： [1]Department of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, West China Hospital, Sichuan University, Chengdu,Sichuan, 610041, China [2]Institute of Respiratory Health, Targeted Tracer Research and Development Laboratory, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, China [3]Precision Medicine Center, Precision Medicine Key Laboratory of Sichuan Province, West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, China [4]The Research Units of West China, Chinese Academy of Medical Sciences, West China Hospital, Chengdu, Sichuan, 610041, China [5]State Key Laboratory of Respiratory Health and Multimorbidity, West China Hospital, Chengdu, Sichuan, 610041, China [6]Department of Radiation Oncology, Radiation Oncology Key Laboratory of Sichuan Province, Sichuan Clinical Research Center for Cancer, Sichuan Cancer Hospital & Institute, Sichuan Cancer Center, Affiliated Cancer Hospital of University of Electronic Science and Technology of China, Chengdu, China [7]Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129,

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关键词： Necroptosis Neuroinflammation RIPK1 Positron emission tomography Radioligands

摘要：

Targeting receptor-interacting protein kinase 1 (RIPK1) has emerged as a promising therapeutic strategy for various neurodegenerative disorders. The development of a positron emission tomography (PET) probe for brain RIPK1 imaging could offer a valuable tool to assess therapeutic effectiveness and uncover the neuropathology associated with RIPK1. In this study, we present the development and characterization of two new PET radioligands, [11C]PB218 and [11C]PB220, which have the potential to facilitate brain RIPK1 imaging. [11C]PB218 and [11C]PB220 were successfully synthesized with a high radiochemical yield (34 % - 42 %) and molar activity (293 - 314 GBq/µmol). PET imaging characterization of two radioligands was conducted in rodents, demonstrating that both newly developed tracers have good brain penetration (maximum SUV = 0.9 - 1.0) and appropriate brain clearance kinetic profiles. Notably, [11C]PB218 has a more favorable binding specificity than [11C]PB220. A PET/MR study of [11C]PB218 in a non-human primate exhibited good brain penetration, desirable kinetic properties, and a safe profile, thus supporting the translational applicability of our new probe. These investigations enable further translational exploration of [11C]PB218 for drug discovery and PET probe development targeting RIPK1.Copyright © 2024 Elsevier Inc. All rights reserved.

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大类 | 2 区

医学

小类 | 1 区有机化学 2 区生化与分子生物学

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无

最新[2023]版：

Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Q1 CHEMISTRY, ORGANIC

影响因子： 4.5 最新[2023版] 4.7 最新五年平均 4.5 出版当年[2023版] 0 出版当年五年平均 4.5 出版前一年[2023版]

第一作者：

第一作者机构： [1]Department of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, West China Hospital, Sichuan University, Chengdu,Sichuan, 610041, China [2]Institute of Respiratory Health, Targeted Tracer Research and Development Laboratory, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, China [3]Precision Medicine Center, Precision Medicine Key Laboratory of Sichuan Province, West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, China [4]The Research Units of West China, Chinese Academy of Medical Sciences, West China Hospital, Chengdu, Sichuan, 610041, China [5]State Key Laboratory of Respiratory Health and Multimorbidity, West China Hospital, Chengdu, Sichuan, 610041, China

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通讯作者：

通讯机构： [1]Department of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, West China Hospital, Sichuan University, Chengdu,Sichuan, 610041, China [2]Institute of Respiratory Health, Targeted Tracer Research and Development Laboratory, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, China [3]Precision Medicine Center, Precision Medicine Key Laboratory of Sichuan Province, West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, China [4]The Research Units of West China, Chinese Academy of Medical Sciences, West China Hospital, Chengdu, Sichuan, 610041, China [5]State Key Laboratory of Respiratory Health and Multimorbidity, West China Hospital, Chengdu, Sichuan, 610041, China [*1]Department of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, China

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Synthesis and preclinical evaluation of 11C-labeled 7-Oxo-2,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridine radioligands for RIPK1 positron emission tomography imaging

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