DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7nM)[1]. DPA-714 has highly specific binding and the ability to penetrate the blood-brain barrier, which enables visualization of inflammatory processes in vivo non-invasively[2]. DPA-714 can be used as a reference substance for detecting 18F-labeled forms, thereby developing the mass spectrometry analysis method for detecting metabolite components[3].
References:
[1] James M L, Fulton R R, Vercoullie J, et al. DPA-714, a new translocator protein–specific ligand: synthesis, radiofluorination, and pharmacologic characterization[J]. Journal of Nuclear Medicine, 2008, 49(5): 814-822.
[2] Cybulska K A, Bloemers V, Perk L R, et al. Optimised GMP-compliant production of [18F] DPA-714 on the Trasis AllinOne module[J]. EJNMMI Radiopharmacy and Chemistry, 2021, 6(1): 20.
[3] Peyronneau M A, Saba W, Goutal S, et al. Metabolism and quantification of [18F] DPA-714, a new TSPO positron emission tomography radioligand[J]. Drug Metabolism and Disposition, 2013, 41(1): 122-131.
DPA-714是一种高亲和力的转运蛋白（TSPO）配体（Ki=7nM）[1]。DPA-714 具有高度特异性结合能力，并且能够穿透血脑屏障，从而能够无创地在体内可视化炎症过程[2]。DPA-714 可用作检测18F标记形式的参考物质，以开发出用于检测代谢物成分的质谱分析方法[3]。