Technetium-99m galactosyl-neoglycoalbumin: preparation and preclinical studies.

摘要: Technetium-99m galactosyl-neoglycoalbumin ([Tc] NGA), a labeled analog ligand to the hepatocyte-specific receptor, hepatic binding protein (HBP), was prepared and tested for labeling yield, stability, biodistribution, toxicity, dosimetry. The synthesized by covalent coupling of carbohydrate bifunctional reagent, 2-imino-2-ethyloxymethyl-1-thiogalactose, human serum albumin. Testing in mice rabbits revealed product be nontoxic apyrogenic. Technetium yields excess 95%, electrolytic method, did not alter molecular weight profile neoglycoalbumin. NGA-bound activity remained stable at least 4 hr. Biodistribution studies demonstrated liver as single focus tracer uptake. Dosimetry based on kinetic three baboons. Absorbed doses liver, small intestine, urinary bladder wall, uterus were 0.089, 0.28, 0.56, 0.88 rad/mCi, respectively. Total body, lens eye, red marrow, ovaries, testes less than 0.06 rad/mCi. High specificity imparted receptor combined with high acceptable dosimetry, safety provide [Tc]NGA attributes required routine clinical assessment hepatocyte function.