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One-step radiosynthesis of 4-[18F]flouro-3-nitro-N-2-propyn-1-yl-benzamide ([18F]FNPB): a new stable aromatic porosthetic group for efficient labeling of peptides with fluorine-18 | |
Li, YS; Liu, YQ; Zhang, L(张岚); Xu, YH | |
2012 | |
Source Publication | JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
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ISSN | 0362-4803 |
Volume | 55Issue:6 |
Abstract | 4-[18F]flouro-3-nitro-N-2-propyn-1-yl-benzamide ([18F]FNPB) was developed as a new stable aromatic prosthetic group for more efficient click labeling of peptides. A new aromatic precursor 3,4-dinitro-N-2-propyn-1-yl-benzamide was radiofluorinated using [18F]KF/K2.2.2 followed by HPLC purification to obtain the desired product [18F]FNPB. [18F]FNPB was synthesized with a 58% radiochemical yield, a specific activity?>?350?GBq/mu mol, and radiochemical purity was exceeded 98% in 40?min. The in vitro stability studies showed no detectable radiodefluorination over 2?h in mouse plasma. The click labeling yield of three different peptides with [18F]FNPB were all above 87%. The in vitro study suggests that [18F]FNPB may be stable?in vivo and could have general application in labeling peptides with high radiochemical yield for positron emission tomography applications. Copyright (c) 2012 John Wiley & Sons, Ltd. |
Language | 英语 |
Funding Project | 应物所项目组 |
WOS ID | WOS:000305510200008 |
Citation statistics | |
Document Type | 期刊论文 |
Identifier | http://ir.sinap.ac.cn/handle/331007/13229 |
Collection | 中科院上海应用物理研究所2011-2020年 |
Recommended Citation GB/T 7714 | Li, YS,Liu, YQ,Zhang, L,et al. One-step radiosynthesis of 4-[18F]flouro-3-nitro-N-2-propyn-1-yl-benzamide ([18F]FNPB): a new stable aromatic porosthetic group for efficient labeling of peptides with fluorine-18[J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS,2012,55(6). |
APA | Li, YS,Liu, YQ,Zhang, L,&Xu, YH.(2012).One-step radiosynthesis of 4-[18F]flouro-3-nitro-N-2-propyn-1-yl-benzamide ([18F]FNPB): a new stable aromatic porosthetic group for efficient labeling of peptides with fluorine-18.JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS,55(6). |
MLA | Li, YS,et al."One-step radiosynthesis of 4-[18F]flouro-3-nitro-N-2-propyn-1-yl-benzamide ([18F]FNPB): a new stable aromatic porosthetic group for efficient labeling of peptides with fluorine-18".JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS 55.6(2012). |
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