Galactosyl neoglycoalbumin (NGA) was synthesized by the covalent coupling of a bifunctional reagent, 2-imino-2-ethyloxymethyl-l-thiogalactose, to human serum albumin. The average number of galactose groups per albumin molecule (Gal/HSA) of NGA was 30. NGA was labeled directly with Na^99m TcO₄. The radiochemical purity of ^99mTc-NGA was over 90%. Consequences of the preclinical studies show that ^99mTc-NGA is a good hepatic receptor imaging agent, uptaken by hepatic cells specifically, and excreted majorly from the biliary system and the gastrointestinal (GI) tract.