Automated radiosynthesis of [11C]MTP38-a phosphodiesterase 7 imaging tracer using [11C]hydrogen cyanide for clinical applications
Automated radiosynthesis of [11C]MTP38-a phosphodiesterase 7 imaging tracer using [11C]hydrogen cyanide for clinical applications
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使用[11C]氰化氢自动放射合成[11C]MTP38-a磷酸二酯酶7成像示踪剂用于临床应用
DOI：
10.1002/jlcr.3965
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发表时间：
2022
影响因子：
1.8
通讯作者：
Oboka
中科院分区：
文献类型：
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作者：
Kawamura Kazunori;Hashimoto Hiroki;Ohkubo Takayuki;Hanyu Masayuki;Ogawa Masanao;Nengaki Nobuki;Arashi Daisuke;Kurihara Yusuke;Fujishiro Tomoya;Togashi Takahiro;Sakai Toshiyuki;Muto Masatoshi;Takei Makoto;Ishii Hideki;Saijo Takeaki;Matsumura Takehiko;Oboka
我们开发了8-氨基-3-（2S，5 R-二甲基-1-哌啶基）-[1，2，4]三唑并[4，3-a]吡嗪-5-[11 C]腈（[11 C] MTP 38）作为磷酸二酯酶7成像的正电子发射断层扫描（PET）示踪剂。为了使[11 C] MTP 38的生产全自动化，常规且有效地用于临床应用，我们确定了使用[11 C]氰化氢（[11 C]HCN）作为PET放射性药物的[11 C] MTP 38的放射性合成程序。在辐照结束后40 min内，使用内部开发的自动11 C标记合成仪进行[11 C] MTP 38的放射合成。[11 C] MTP 38具有相对较高的放射化学产率（在辐射结束时基于[11 C] CO2为33 ± 5.5%，衰变校正，n= 15），放射化学纯度（> 97%，n = 15）和摩尔活性（在合成结束时为47 ± 12 GBq/μmol，n= 15）。[11 C] MTP 38注射液的所有质量控制（QC）检测结果均符合我们的内部QC和质量保证质量标准。我们使用11 C标记合成仪和无菌隔离器成功地自动化了[11 C] MTP 38的放射合成，用于临床应用。总之，该方案提供了一种适合临床应用的新型放射性药物[11 C] MTP 38。
We have developed 8‐amino‐3‐(2S,5R‐dimethyl‐1‐piperidyl)‐[1,2,4]triazolo[4,3‐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 automated11C‐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]CO2at 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 an11C‐labeling synthesizer and sterile isolator. Taken together, this protocol provides a new radiopharmaceutical [11C]MTP38 suitable for clinical applications.