Development of Mitochondria-Targeted Small-Molecule Dyes for Myocardial PET and Fluorescence Bimodal Imaging
文献类型：期刊论文
| 作者 | Zheng, Lingling1,2; Wang, Zhiming1; Zhang, Xiaoqing1,2; Zhou, Yujing1,2; Ji, Aiyan1; Lou, Hongyue1; Liu, Xingdang2; Chen, Hao1; Cheng, Zhen1,2,3 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2022-01-13 |
| 卷号 | 65期号:1页码:497-506 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.1c01660 |
| 通讯作者 | Liu, Xingdang(xingdliu@fudan.edu.cn) ; Chen, Hao(haoc@simm.ac.cn) ; Cheng, Zhen(zcheng@simm.ac.cn) |
| 英文摘要 | Mitochondria-targeting positron emission tomography (PET) and fluorescent dual-modal probes are rarely reported. As one of the most promising lipophilic cations, F16 and its derivatives (F16s) have never been used for myocardial imaging. In this work, 14 F16s are synthesized and evaluated for cardiac imaging. In vitro cell fluorescence imaging revealed that the lead probe 5MEF is precisely localized in the mitochondria of cardiomyocytes. In addition, it shows excellent ex vivo fluorescence imaging quality with the heart-to-muscle and heart- to- liver ratios up to similar to 2. Furthermore, the radiofluorinated probe F-18-5MEF is successfully prepared and shows a high initial heart uptake of 8.66 +/- 0.34 % ID/g at 5 min post injection. It displays a high heart imaging performance, a long retention time in the heart, and a low background in the most normal tissues as revealed by PET. To our knowledge, this is the first time novel F16 analogues are designed and developed for myocardial dual-modal imaging. |
| WOS关键词 | F-18-FLUOROBENZYL TRIPHENYL PHOSPHONIUM ; TRIPHENYLPHOSPHONIUM CATION ; POTENTIAL AGENT ; VOLTAGE SENSOR ; BLOOD-FLOW ; DELINEATION ; TRACERS ; SYSTEM |
| 资助项目 | Shanghai Municipal Science and Technology Major Project ; National Key R&D Program of China[2021ZD0203900] ; National Natural Science Foundation of China[82071976] ; Shanghai Pujiang Program[19PJ1411100] ; National Key Research and Development Plan Digital Diagnosis and Treatment Equipment Research and Development Project[2017YFC0113300] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | AMER CHEMICAL SOC |
| WOS记录号 | WOS:000766544600028 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/300203]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Liu, Xingdang; Chen, Hao; Cheng, Zhen |
| 作者单位 | 1.Chinese Acad Sci, Mol Imaging Ctr, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Fudan Univ, Huashan Hosp, Dept Nucl Med, Shanghai 200040, Peoples R China 3.Bohai Rim Adv Res Inst Drug Discovery, Yantai 264000, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zheng, Lingling,Wang, Zhiming,Zhang, Xiaoqing,et al. Development of Mitochondria-Targeted Small-Molecule Dyes for Myocardial PET and Fluorescence Bimodal Imaging[J]. JOURNAL OF MEDICINAL CHEMISTRY,2022,65(1):497-506. |
| APA | Zheng, Lingling.,Wang, Zhiming.,Zhang, Xiaoqing.,Zhou, Yujing.,Ji, Aiyan.,...&Cheng, Zhen.(2022).Development of Mitochondria-Targeted Small-Molecule Dyes for Myocardial PET and Fluorescence Bimodal Imaging.JOURNAL OF MEDICINAL CHEMISTRY,65(1),497-506. |
| MLA | Zheng, Lingling,et al."Development of Mitochondria-Targeted Small-Molecule Dyes for Myocardial PET and Fluorescence Bimodal Imaging".JOURNAL OF MEDICINAL CHEMISTRY 65.1(2022):497-506. |
入库方式： OAI收割
来源：上海药物研究所
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