18F-FBEM-NGA的合成及结构表征

Synthesis and Characterization of 18F-FBEM-NGA as a Potential ASGP Receptor Imaging Agent

  • 摘要:18F-FBEM对新乳糖白蛋白(NGA)进行标记,探讨标记辅助基团标记蛋白或多肽的可行性。用18F-SFB与N-(2-氨基乙基)马来酰亚胺三氟乙酸盐反应合成了一种用于正电子发射计算机断层显像(PET)药物的辅助基团18F-FBEM,并进一步制得18F-FBEM-NGA。18F-FBEM的标记时间为2.5 h,经衰变校正后的放化产率为9.8%。18F-FBEM-NGA的放化产率为15.9%,放化纯度>98%,体外可稳定放置3.5 h。实验结果表明,18F-FBEM中的马来酰亚胺双键可在室温下与巯基发生高效率反应,可用于标记含巯基的多肽或蛋白分子等。

     

    Abstract: A 18F-labelling prosthetic group named as N-2-(4-18F-fluorobenzamido) ethyl maleimide (18F-FBEM) was prepared for peptides and protein labeling, and the radiopharmaceuticals prepared from this prosthetic group were designed for positron emission tomography (PET) imaging. This prosthetic group was synthesized by the reaction of Nsuccinimidyl 4-18F-fluorobenzoate (18F-SFB) with N-(2-aminoethyl) maleimide trifluoroacetate salt. The total synthesis time from 18F- to 18F-FBEM was about 2.5 h with decay corrected radiolabeling yield of 9.8%. The double bond contained in maleimide of the synthon can react with sulfhydryl groups with high efficiency under room temperature, thus it can be applied in indirect radiofluorinations of thiol-containing molecules such as peptides and protein. 18F-labeled galactosyl-neoglycoalbumin (18F-FBEM-NGA) was developed based on 18F-FBEM for example.

     

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