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Automated radiosynthesis of [11C]MTP38—a phosphodiesterase 7 imaging tracer—using [11C]hydrogen cyanide for clinical applications |
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| Authors: | Kazunori Kawamura Hiroki Hashimoto Takayuki Ohkubo Masayuki Hanyu Masanao Ogawa Nobuki Nengaki Daisuke Arashi Yusuke Kurihara Tomoya Fujishiro Takahiro Togashi Toshiyuki Sakai Masatoshi Muto Makoto Takei Hideki Ishii Takeaki Saijo Takehiko Matsumura Naoyuki Obokata Ming-Rong Zhang |
| Institution: | 1. Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, Chiba, Japan;2. Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, Chiba, Japan
SHI Accelerator Service Ltd., Tokyo, Japan;3. Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science, National Institutes for Quantum Science and Technology, Chiba, Japan Tokyo Nuclear Services Ltd., Tokyo, Japan;4. Sohyaku Innovative Research Division, Mitsubishi Tanabe Pharma Corporation, Yokohama, Japan |
| Abstract: | We have developed 8-amino-3-(2S,5R-dimethyl-1-piperidyl)-1,2,4]triazolo4,3-a]pyrazine-5-11C]carbonitrile (11C]MTP38) as a positron emission tomography (PET) tracer for the imaging of phosphodiesterase 7. For the fully automated production of 11C]MTP38 routinely and efficiently for clinical applications, we determined the radiosynthesis procedure of 11C]MTP38 using 11C]hydrogen cyanide (11C]HCN) as a PET radiopharmaceutical. Radiosynthesis of 11C]MTP38 was performed using an automated 11C-labeling synthesizer developed in-house within 40 min after the end of irradiation. 11C]MTP38 was obtained with a relatively high radiochemical yield (33 ± 5.5% based on 11C]CO2 at the end of irradiation, decay-corrected, n = 15), radiochemical purity (>97%, n = 15), and molar activity (47 ± 12 GBq/μmol at the end of synthesis, n = 15). All the results of the quality control (QC) testing for the 11C]MTP38 injection complied with our in-house QC and quality assurance specifications. We successfully automated the radiosynthesis of 11C]MTP38 for clinical applications using an 11C-labeling synthesizer and sterile isolator. Taken together, this protocol provides a new radiopharmaceutical 11C]MTP38 suitable for clinical applications. |
| Keywords: | [11C]hydrogen cyanide [11C]MTP38 carbon-11 phosphodiesterase 7 positron emission tomography quality control testing radiosynthesis |