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Development of a novel 18F-labeled reversible-binding radioligand for imaging monoacylglycerol lipase with positron emission tomography
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Acta Pharmaceutica Sinica B | 2025, 15(12) : 6714 - 6726
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Acta Pharmaceutica Sinica B | 2025, 15(12): 6714-6726
• Original articles •
Development of a novel 18F-labeled reversible-binding radioligand for imaging monoacylglycerol lipase with positron emission tomography
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Published: 2025-12-25 doi: 10.1016/j.apsb.2025.05.041
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Monoacylglycerol lipase (MAGL) constitutes a crucial serine hydrolase within the endocannabinoid system, which has been suggested as a potential therapeutic target for the treatment of various neurodegenerative disorders. While MAGL inhibitors have entered the clinical arena, a highly selective and MAGL-specific positron emission tomography (PET) ligand holds promise to significantly facilitate clinical drug development by allowing the quantification of MAGL levels and the assessment of target occupancy in patients. Accordingly, this study aimed to develop a new series of reversible MAGL inhibitor candidates, based on a piperazinyl azetidine diamide scaffold. Compound 3 demonstrated the most promising performance characteristics in pharmacological evaluations compared to other MAGL inhibitor candidates. Subsequently, it was labeled with fluorine-18 and further assessed through autoradiography and PET imaging, as well as ex vivo biodistribution and metabolite analysis experiments in rodents. Compound 3 exhibited a heterogeneous radioactivity distribution, favorable brain uptake, and excellent in vivo binding specificity. Target occupancy studies with a therapeutic MAGL inhibitor demonstrated a dose-dependent PET signal reduction of [18F]3 in rat brains. In conclusion, [18F]3 ([18F]MAGL-2011) has the potential to serve as an effective MAGL PET ligand.
Monoacylglycerol lipase  /  MAGL  /  Serine hydrolase  /  PET
. Development of a novel ¹⁸F-labeled reversible-binding radioligand for imaging monoacylglycerol lipase with positron emission tomography. 药学学报（英文版）, 2025 , 15 (12) : 6714 -6726 . DOI: 10.1016/j.apsb.2025.05.041
. Development of a novel 18F-labeled reversible-binding radioligand for imaging monoacylglycerol lipase with positron emission tomography[J]. Acta Pharmaceutica Sinica B, 2025 , 15 (12) : 6714 -6726 . DOI: 10.1016/j.apsb.2025.05.041
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Year 2025 volume 15 Issue 12
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doi: 10.1016/j.apsb.2025.05.041
  • Receive Date：2024-10-28
  • Online Date：2026-10-25
  • Published：2025-12-25
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  • Received：2024-10-28
  • Revised：2025-01-22
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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