{"title":"新型肿瘤缺氧显像剂:[99mTc]Tc(CO)3-CPA-2-NIM。","authors":"Xiao Lin, Xiaojie Tan, Fengyu Wu, Qian Yu","doi":"10.2174/1874471016666230320144641","DOIUrl":null,"url":null,"abstract":"<p><strong>Introduction: </strong>Hypoxia imaging agents can selectively remain in hypoxic tissue, which can directly reflect the location and degree of hypoxia.</p><p><strong>Methods: </strong>Synthesized a novel tumor hypoxia imaging probe [<sup>99m</sup>Tc]Tc(CO)<sub>3</sub>-CPA-2-NIM and evaluated its biological behavior with the purpose to assess its possibility of becoming a qualified tumor hypoxia imaging agent.</p><p><strong>Results: </strong>Radiochemcial purity of [<sup>99m</sup>Tc]Tc(CO)<sub>3</sub>-CPA-2-NIM was greater than 95% after HPLC purification. Lipophilicity coefficient of this complex was -1.74 ± 0.10 (n = 5, number of experiments), indicating it was a hydrophilic complex. <i>In vitro</i> cell experiments demonstrated that this complex has selectivity for hypoxia at oxygen concentrations < 10 ppm (parts per million). Biodistribution experiment in S180 tumor bearing mice showed that tumor uptake reached its highest at 2 h post-injection with mice tumor-to-muscle ratio.</p><p><strong>Conclusions: </strong>Complex [<sup>99m</sup>Tc]Tc(CO)<sub>3</sub>-CPA-2-NIM has the possibility of becoming a tumor hypoxia imaging agent.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":"16 4","pages":"300-307"},"PeriodicalIF":1.5000,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"A Novel Tumor Hypoxia Imaging Agent: [<sup>99m</sup>Tc]Tc(CO)<sub>3</sub>-CPA-2-NIM.\",\"authors\":\"Xiao Lin, Xiaojie Tan, Fengyu Wu, Qian Yu\",\"doi\":\"10.2174/1874471016666230320144641\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Introduction: </strong>Hypoxia imaging agents can selectively remain in hypoxic tissue, which can directly reflect the location and degree of hypoxia.</p><p><strong>Methods: </strong>Synthesized a novel tumor hypoxia imaging probe [<sup>99m</sup>Tc]Tc(CO)<sub>3</sub>-CPA-2-NIM and evaluated its biological behavior with the purpose to assess its possibility of becoming a qualified tumor hypoxia imaging agent.</p><p><strong>Results: </strong>Radiochemcial purity of [<sup>99m</sup>Tc]Tc(CO)<sub>3</sub>-CPA-2-NIM was greater than 95% after HPLC purification. Lipophilicity coefficient of this complex was -1.74 ± 0.10 (n = 5, number of experiments), indicating it was a hydrophilic complex. <i>In vitro</i> cell experiments demonstrated that this complex has selectivity for hypoxia at oxygen concentrations < 10 ppm (parts per million). Biodistribution experiment in S180 tumor bearing mice showed that tumor uptake reached its highest at 2 h post-injection with mice tumor-to-muscle ratio.</p><p><strong>Conclusions: </strong>Complex [<sup>99m</sup>Tc]Tc(CO)<sub>3</sub>-CPA-2-NIM has the possibility of becoming a tumor hypoxia imaging agent.</p>\",\"PeriodicalId\":10991,\"journal\":{\"name\":\"Current radiopharmaceuticals\",\"volume\":\"16 4\",\"pages\":\"300-307\"},\"PeriodicalIF\":1.5000,\"publicationDate\":\"2023-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current radiopharmaceuticals\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.2174/1874471016666230320144641\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current radiopharmaceuticals","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/1874471016666230320144641","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
A Novel Tumor Hypoxia Imaging Agent: [99mTc]Tc(CO)3-CPA-2-NIM.
Introduction: Hypoxia imaging agents can selectively remain in hypoxic tissue, which can directly reflect the location and degree of hypoxia.
Methods: Synthesized a novel tumor hypoxia imaging probe [99mTc]Tc(CO)3-CPA-2-NIM and evaluated its biological behavior with the purpose to assess its possibility of becoming a qualified tumor hypoxia imaging agent.
Results: Radiochemcial purity of [99mTc]Tc(CO)3-CPA-2-NIM was greater than 95% after HPLC purification. Lipophilicity coefficient of this complex was -1.74 ± 0.10 (n = 5, number of experiments), indicating it was a hydrophilic complex. In vitro cell experiments demonstrated that this complex has selectivity for hypoxia at oxygen concentrations < 10 ppm (parts per million). Biodistribution experiment in S180 tumor bearing mice showed that tumor uptake reached its highest at 2 h post-injection with mice tumor-to-muscle ratio.
Conclusions: Complex [99mTc]Tc(CO)3-CPA-2-NIM has the possibility of becoming a tumor hypoxia imaging agent.
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