Preclinical evaluation of 99mTc-histidine as a possible tumor imaging agent

Abstract

Radiolabeling of histidine (Hist), an essential amino acid, with ^99mTc was performed. The radiochemical yield higher than 95% was achieved with stannous chloride as a reducing agent. Factors affecting the radiochemical yield (histidine amount, stannous chloride amount, reaction time, pH of the reaction mixture) were studied in detail, and the reaction conditions were optimized. In vitro stability of the radiolabeled complex was checked, and it was found to be stable for up to 6 h. ^99mTc-Hist was injected intravenously into normal and tumor-bearing mice. Biodistribution studies revealed that the ^99mTc-Hist uptake in tumor sites was 10 and 16% ID/g in ascites and 7 and 9.2% ID/g in thigh solid tumor at 60 and 120 min post injection, respectively. The amount of ^99mTc-Hist in ascites and solid tumor increased with time and then decreased slowly. Thus, ^99mTc-Hist can be used as a potential agent for imaging tumor sites.