首页> 外国专利> 18 Radiotracer introduced 18Ffluoromethyl group targeting neuroinflammation for PET imaging and Synthesis of Radiotracer and its biological evaluation Method for Radiotracer introduced 18Ffluoromethyl group targeting neuroinflammation for PET imaging

18 Radiotracer introduced 18Ffluoromethyl group targeting neuroinflammation for PET imaging and Synthesis of Radiotracer and its biological evaluation Method for Radiotracer introduced 18Ffluoromethyl group targeting neuroinflammation for PET imaging

机译：[18] Radiotracer引入了[18F]氟甲基靶向神经炎症用于PET成像和Radiotracer的合成及其生物学评价方法，Raditracer引入了[18F]氟甲基靶向神经炎症用于PET成像。

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TECHNICAL FIELD The present invention relates to a neuroinflammatory target proton emission tomography radiotracer having an [18F] fluoromethyl group introduced therein, a method of synthesizing the same, and a biological evaluation method using the same. The present invention relates to a method for evaluating a biological result using PBR28- [18F] fluoroiodomethane labeled with -18 was introduced in two steps, or fluorine-18 was substituted in one step and a high yield using a triazolium triflate precursor to introduce a fluoromethyl group Fluorine-18 labeled radioactive tracer was prepared. As a result of pharmacokinetic comparison in the known [ ¹¹ C] PBR28 and in vitro binding affinity, fat affinity and cranial nerve inflammation model, the fluorine-18 labeled radioactive tracker with [ ¹¹ C] PBR28 showed similar binding affinity Lipid affinity. In addition, the PET image comparison evaluation in the cranial nerve inflammation model confirmed fluoro-18 labeled radioactive trackers with fluoromethyl groups were superior to selective / specific uptake in the inflammatory area at a faster time, High stability was confirmed. According to the present invention, in the synthesis of a fluorine-18 labeled radioactive tracer into which a fluoromethyl group for a new cranial nerve inflammatory target PET is introduced and fluorine-18 having a relatively longer half-life than [ ¹¹ C] PBR28 in the diagnosis of cranial nerve inflammatory disease, It is expected to be a radioactive tracer for cranial nerve inflammation target PET, which can be effectively labeled by structural changes, and has excellent selective, specific imaging and pharmacokinetic advantages.

机译：导入有[18 F]氟甲基的神经炎性靶质子发射体层摄影放射示踪剂，其合成方法以及使用其的生物评价方法技术领域本发明涉及导入有[18 F]氟甲基的神经炎性靶质子发射体层摄影放射示踪剂，其合成方法以及使用其的生物学评价方法。本发明涉及一种评估生物学结果的方法，该方法使用两步引入以-18标记的PBR28- [18F]氟碘甲烷，或一步取代氟18并使用三氟甲磺酸三唑鎓前体引入高收率。氟甲基制备了氟18标记的放射性示踪剂。根据已知的[^{11 C] PBR28的药代动力学比较，以及体外结合亲和力，脂肪亲和力和颅神经炎症模型，用[^{11 C] PBR28显示出相似的结合亲和力脂质亲和力。另外，在颅神经炎症模型中的PET图像比较评估证实，具有氟甲基基团的氟18标记的放射性示踪剂在较快的时间内在炎症区域中的选择性/特异性摄取更好，并证实了高稳定性。根据本发明，在氟18标记的放射性示踪剂的合成中，其中引入了用于新的颅神经炎性靶标PET的氟甲基，并且氟-18具有比[^{11 < [Sup> C] PBR28在颅神经炎性疾病的诊断中，有望成为一种针对颅神经炎性靶PET的放射性示踪剂，它可以通过结构变化进行有效标记，并具有出色的选择性，特异性成像和药代动力学优势。}}}

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公开/公告号KR101602912B1

专利类型
公开/公告日2016-03-11

原文格式PDF
申请/专利权人 주식회사 바이오이미징코리아;
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申请/专利号KR20130110282
发明设计人 이병철;문병석;정재호;
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申请日2013-09-13
分类号A61K51/04;A61K51/02;A61P29;
国家 KR
入库时间 2022-08-21 14:12:48

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