| 新型~(18)F标记心肌灌注显像剂的PET显像实验研究; The preliminary experimental study of a novel ~(18)F-labeled myocardial perfusion imaging agent for PET imaging | |
| 王道宇 ; 牟甜甜 ; 赵祚全 ; 郭风 ; 张现忠 ; 方纬 | |
| 2015-06-15 | |
| 关键词 | 18F-FPTP2 哒嗪酮 心肌灌注 发射型正电子断层显像 [18F]FPTP2 Pyridazinone Myocardial perfusion Positron emission tomography imaging |
| 英文摘要 | 目的:通过初步动物实验,评价4-氯-2-叔丁基-5-[[6-[[4-(2-氟-18f-乙基)-1H-1,2,3-三唑-1-基]甲基]-2-吡啶基]甲氧基]-3(2H)-哒嗪酮(18f-fPTP2)用于心肌灌注发射型正电子断层显像(PET)的可能性。方法:采用18f-f-取代OTS前体的方法进行标记,通过HPlC非梯度洗脱进行纯化,并通过HPlC确认标记化合物结构。中华小型猪经静脉注射18f-fPTP2(37MbQ/15 kg),并于注射后2 MIn、10 MIn、20 MIn、30 MIn、40 MIn、50 MIn和60 MIn分别进行PET/CT扫描。结果:18f-fPTP2制备的总时间为70 MIn,未校正的放化产率为(25±7.2)%,放射化学纯度>98%。PET研究表明,18f-fPTP2在中华小型猪中的心肌摄取随时间的延长而增加,靶器官与非靶器官比值亦随之增加。注射后2 MIn,心和(或)肝以及心和(或)肺放射性摄取比值分别为0.65±0.10和3.47±0.29。注射后60 MIn,心和(或)肝以及心和(或)肺放射性摄取比值分别为0.92±0.13和9.28±0.77。结论:18f-fPTP2能够被心肌组织摄取而显影清晰,但心和(或)肝放射性摄取比值需要进一步提高。; Objective: To preliminarily evaluate the potential of 2-tert-butyl-4-chloro-5-((6-((4-(2-[18F]fluroethyl)-1H-1,2,3-triazol-1-yl)methyl)-2-pyridinyl)methoxy)-3(2H)-pyridazinone([18F]FPTP2) as a myocardial perfusion imaging agent, by animal positron emission tomography(PET) imaging.Methods: [18F]FPTP2 was prepared by substituting tosyl of precursor with 18 F, purified and confirmed by HPLC.[18F]FPTP2(37 MBq/15 kg) was injected into Chinese mini-swines intravenously by a venous catheter.The cardiac PET scans were performed at 2, 10, 20, 30, 40, 50 and 60 min after injection.Results: The total radio-synthesis time was 70 min, radiochemical yield was 25±7.2% without correction.The radiochemical purities(RCP) were >98% after purification.In PET imaging study, the heart uptake and target-to-nontarget uptake ratios increased with time.The heart/liver and heart/lung ratios were 0.65±0.10 and 3.47±0.29 at 2 min post injection, 0.92±0.13 and 9.28±0.77 at 60 min post injection respectively.Conclusion: Although the higher uptake of [18F]FPTP2 were shown in myocardium, the heart/liver ratio still need to be improved in future study.; 国家自然科学基金(81301251)“新型氟-18标记的哒嗪酮类心肌灌注显像剂的研制及PET显像实验研究” |
| 语种 | zh_CN |
| 内容类型 | 期刊论文 |
| 源URL | [http://dspace.xmu.edu.cn/handle/2288/102279]  |
| 专题 | 公共卫生－已发表论文 |
| 推荐引用方式 GB/T 7714 | 王道宇,牟甜甜,赵祚全,等. 新型~(18)F标记心肌灌注显像剂的PET显像实验研究, The preliminary experimental study of a novel ~(18)F-labeled myocardial perfusion imaging agent for PET imaging[J],2015. |
| APA | 王道宇,牟甜甜,赵祚全,郭风,张现忠,&方纬.(2015).新型~(18)F标记心肌灌注显像剂的PET显像实验研究.. |
| MLA | 王道宇,et al."新型~(18)F标记心肌灌注显像剂的PET显像实验研究".(2015). |
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