Synthesis of [ 11 C]carbonyl-labeled cyclohexyl (5-(2-acetamidobenzo[d]thiazol-6-yl)-2-methylpyridin-3-yl)carbamate ([ 11 C-carbonyl]PK68) as a potential PET tracer for receptor-interacting protein 1 kinase.
Autor: | Yamasaki T; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan., Kumata K; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan., Hiraishi A; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan., Zhang Y; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan., Wakizaka H; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan., Kurihara Y; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan.; SHI Accelerator Service Co. Ltd., 1-17-6 Osaki, Shinagawa-ku, Tokyo, 141-0032, Japan., Nengaki N; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan.; SHI Accelerator Service Co. Ltd., 1-17-6 Osaki, Shinagawa-ku, Tokyo, 141-0032, Japan., Zhang MR; Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology, 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan. zhang.ming-rong@qst.go.jp. |
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Jazyk: | angličtina |
Zdroj: | EJNMMI radiopharmacy and chemistry [EJNMMI Radiopharm Chem] 2022 Mar 15; Vol. 7 (1), pp. 4. Date of Electronic Publication: 2022 Mar 15. |
DOI: | 10.1186/s41181-022-00156-1 |
Abstrakt: | Background: Receptor-interacting protein 1 kinase (RIPK1) is a key enzyme in the regulation of cellular necroptosis. Recently, cyclohexyl (5-(2-acetamidobenzo[d]thiazol-6-yl)-2-methylpyridin-3-yl)carbamate (PK68, 5) has been developed as a potent inhibitor of RIPK1. Herein, we synthesized [ 11 C]carbonyl-labeled PK68 ([ 11 C-carbonyl]PK68, [ 11 C]PK68) as a potential PET tracer for imaging RIPK1 and evaluated its brain uptake in vivo. Results: We synthesized [ 11 C]PK68 by reacting amine precursor 14 with [ 11 C]acetyl chloride. At the end of synthesis, we obtained [ 11 C]PK68 of 1200-1790 MBq with a radiochemical yield of 9.1 ± 5.9% (n = 10, decay-corrected to the end of irradiation) and radiochemical purity of > 99%, and a molar activity of 37-99 GBq/μmol starting from 18-33 GBq of [ 11 C]CO Conclusions: In the present study, we successfully radiosynthesized [ 11 C]PK68 as a potential PET tracer and evaluated its brain uptake. We are planning to optimize the chemical structure of [ 11 C]PK68 and conduct further PET studies on it using pathological models. (© 2022. The Author(s).) |
Databáze: | MEDLINE |
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