首页> 外国专利> HEXA-LACTOSIDE-TRIAZANONANE TRIACETIC ACID (NOTA) DERIVATIVE, METHOD FOR RADIOLABELING HEXA-LACTOSIDE POSITRON EMISSION TOMOGRAPHY (PET) IMAGING AGENT FOR LIVER RECEPTOR WITH GA-68, AND HEXA-LACTOSIDE PET IMAGING AGENT FOR LIVER RECEPTOR

HEXA-LACTOSIDE-TRIAZANONANE TRIACETIC ACID (NOTA) DERIVATIVE, METHOD FOR RADIOLABELING HEXA-LACTOSIDE POSITRON EMISSION TOMOGRAPHY (PET) IMAGING AGENT FOR LIVER RECEPTOR WITH GA-68, AND HEXA-LACTOSIDE PET IMAGING AGENT FOR LIVER RECEPTOR

机译:己-乳糖苷-三氮杂壬烷三乙酸(NOTA)衍生物,用GA-68放射标记肝受体正电子发射断层显像(PET)成像剂的方法以及用于肝受体的己交酯PET成像剂

摘要

The present invention provides a hexa-lactoside-triazanonane triacetic acid (NOTA) derivative, a method for radiolabeling a hexa-lactoside positron emission tomography (PET) imaging agent for a liver receptor with Ga-68, and a hexa-lactoside PET imaging agent for a liver receptor. The hexa-lactoside-NOTA derivative is a conjugate of six chains of lactose with NOTA obtained by conjugating hexa-lactoside to a chelating agent p-thiocyanate-benzyl-triazanonane diacetic acid-glutamic acid in the presence of triethyl amine/dimethyl formamide as a solvent. The radiolabeling method comprises labeling with Ga-68 at room temperature. According to the present invention, the labeling effect is stable, the labeling efficiency of the labeled product is greater than 95%, the labeled product is highly stable and the radiochemical purity is still greater than 90% after 4 hours.
机译:本发明提供了六-乳糖苷-三氮杂壬烷三乙酸(NOTA)衍生物,用Ga-68放射性标记用于肝脏受体的六-乳糖苷正电子发射断层成像(PET)成像剂和六-乳糖苷PET成像剂的方法。用于肝脏受体。六乳糖苷-NOTA衍生物是六链乳糖与NOTA的共轭物,是通过在三乙胺/二甲基甲酰胺的存在下将六乳糖苷与螯合剂对硫氰酸酯-苄基-三氮杂双环烷二乙酸-谷氨酸共轭而获得的。溶剂。放射性标记方法包括在室温下用Ga-68标记。根据本发明,标记作用是稳定的,标记产物的标记效率大于95%,标记产物高度稳定,并且放射化学纯度在4小时后仍大于90%。

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