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99mTc-Hydrazinonicotinamide-galactosyl-chitosan.

Authors

Leung K1.

Source

Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2009 Sep 15 [updated 2009 Dec 02].

Author information

1
National for Biotechnology Information, NLM, NIH, Bethesda, MD

Excerpt

Asialoglycoprotein (ASGP) is specifically taken into mammalian hepatocytes by binding to ASGP receptors (ASGP-Rs) (1). The galactosyl moiety of ASGP is recognized on the surface of hepatocytes and is bound by ASGP-R. The ASGP–ASGP-R complex on the cell surface is subsequently taken into cytoplasm by endocytosis and transferred to lysosomes. ASGP-R is then dissociated from ASGP and recycled to the cell surface. ASGP is degraded in the lysosomes and excreted into the bile. The number of ASGP-Rs on the hepatocytes of individuals with liver disease decreases and is thus considered a good indicator for the evaluation of liver function. Because ASGP-R recognizes galactose, 99mTc-diethylenetriamine pentaacetic acid-galactosyl-human serum albumin (99mTc-GSA) (2, 3) and 99mTc-galactosyl-neoglycoalbumin (99mTc-NGA) (4) are ASGP-R probes that accumulate specifically in the liver and are used for liver scintigraphy to determine liver mass and function. Chitosan is a linear polysaccharide composed of D-glucosamine and N-acetylglucosamine subunits with numerous amine groups of D-glucosamine for ligand conjugation. Kim et al. (5) conjugated hydrazinonicotinamide (HYNIC) and galactose (via lactobionic acid) to deacetylate chitosan for radiolabeling with 99mTc to form 99mTc-HYNIC-galactosyl-chitosan (99mTc-HGC) for imaging ASGP-R expression in the liver.

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