Preparation method of 99mTc labeled hydrazinonicotinamide group-pteroyllysine coordination compound

Abstract

The invention discloses a 99mTc labeled hydrazinonicotinamide group-pteroyllysine coordination compound with an expression of 99mTc (HYNIC-Lys-Pteroyl)(Tricine)(TPPTS), a preparation method and application. The target coordination compound is obtained through the following two steps of: (a) synthesizing pteroyllysine 6-(2-N,N-dimethylbenzaldehydehydrazono) niacin as a ligand; and (b) obtaining the 99mTc labeled hydrazinonicotinamide group-pteroyllysine coordination compound. The coordination compound has the advantages of high radiochemical purity, good stability, low price, high tumor uptakerate, good retention and good target/non-target specific values of tumor/blood, tumor/muscle, and the like and can be popularized and applied by being used as a novel 99mTc labeled folate receptor tumor image developer.

Description

Technical field [0001] The present invention relates to 99m The field of Tc-labeled radiopharmaceutical chemistry and clinical nuclear medicine technology, specifically relates to a 99m Preparation method of Tc-labeled hydrazinonicotinyl-pteroyl lysine complex. Background technique [0002] As we all know, folic acid is the abbreviation of pteroyl glutamic acid, also known as vitamin M and vitamin BC. Its molecular structure formula shows that its molecule is composed of three parts: pteridine, p-aminobenzoic acid and L-glutamic acid, and the structure includes α and γ carboxyl groups. The folate receptor is a membrane glycoprotein linked by glycosyl-phosphatidylinositl, with a molecular weight of 38-40kD. The folate receptor is low expressed in normal healthy cells, but in many malignant cells derived from epithelial tissue Tumors, such as ovarian cancer, breast cancer, endometrial cancer, lung cancer, nasopharyngeal cancer and other tumors, are highly expressed. With the...

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Problems solved by technology

Literature report 99m Tc-HYNIC-folate has good target-to-non-target ratios such as tumor / blood, tumor / meat, etc., but the absolute tumor uptake value in the KB tumor-bearing mouse model is low, and the background of liver, spleen, etc. is high ( W. Guo, G. H. Hinkle, R. J. Lee, 99m Tc-HYNIC-folate: a novel receptor-based targeted radiopharmaceutical for tumor imaging. J Nucl Med1999; 40: 1563-1569; Liu Liqin, Wang Shizhen, etc. Folate receptor tumor imaging agent 99m Synthesis and animal imaging of Tc-hydrazinyl nicotinamide hydrazide-folic acid. Chinese Academy of Medical Sciences Journal. 2006; 28:786-789 Chinese Academy of Medical Sciences Journal)

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