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Tytuł:
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Efficient and automatic synthesis of TSPO PET ligand [ F]-GE-180 and its application in rheumatoid arthritis model.
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Autorzy:
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Zhu XX; Department of Nuclear Medicine, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, 230001, Anhui, China.
He YL; School of Pharmacy, Bengbu Medical College, Bengbu, 233030, Anhui, China.
Xie JK; Department of Nuclear Medicine, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, 230001, Anhui, China.
Wang KX; Department of Nuclear Medicine, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, 230001, Anhui, China.
Wang SC; Department of Nuclear Medicine, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, 230001, Anhui, China.
Xie Q; Department of Nuclear Medicine, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, 230001, Anhui, China; School of Pharmacy, Bengbu Medical College, Bengbu, 233030, Anhui, China. Electronic address: .
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Źródło:
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Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine [Appl Radiat Isot] 2022 Jun; Vol. 184, pp. 110213. Date of Electronic Publication: 2022 Mar 23.
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Typ publikacji:
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Journal Article
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Język:
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English
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Imprint Name(s):
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Original Publication: Oxford ; New York : Pergamon Press, c1993-
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MeSH Terms:
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Arthritis, Rheumatoid*/diagnostic imaging
Positron-Emission Tomography*/methods
Animals ; Carbazoles ; Carrier Proteins/metabolism ; Inflammation ; Ligands ; Positron Emission Tomography Computed Tomography ; Rats ; Receptors, GABA-A/metabolism
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Contributed Indexing:
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Keywords: Automated radiosynthesis; RA; TSPO; [(18)F]-GE-180
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Substance Nomenclature:
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0 (Carbazoles)
0 (Carrier Proteins)
0 (GE-180)
0 (Ligands)
0 (Receptors, GABA-A)
141440-82-6 (Tspo protein, rat)
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Entry Date(s):
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Date Created: 20220329 Date Completed: 20220413 Latest Revision: 20220413
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Update Code:
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20240104
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DOI:
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10.1016/j.apradiso.2022.110213
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PMID:
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35349890
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Rheumatoid arthritis (RA) is a common autoimmune disease characterized by chronic synovial inflammation, which ultimately leads to joint deformity and dysfunction. [ 18 F]-GE-180 is a specific PET tracer of the 18 kDa translocator protein (TSPO), which is overexpressed on activated macrophages, and proposed as a biomarker of inflammation. Our study addresses the need to streamline the automatic synthesis of [ 18 F]-GE-180 to make it more accessible for routine production and widespread clinical evaluation and application. The nucleophilic radiofluorination was performed on an AllinOne synthesis module by SPE purification method, and the formulated [ 18 F]-GE-180 was obtained in non-decay corrected radiochemical yields of 69 ± 1.8% in 32 min. PET/CT imaging in animal model showed that [ 18 F]-GE-180 highly concentrated in joints from RA rats. This methodology facilitates efficient synthesis of [ 18 F]-GE-180 in a commercially available synthesis module and shows potential diagnosis performance in RA models.
(Copyright © 2022 Elsevier Ltd. All rights reserved.)
