Abstract

The myocardial imaging agent technetium-99m-hexakis (tertiarybutylisonitrile) ( 99mTc-TBI) was prepared by the reaction of [ 99mTc]pertechnetate with TBI in 50% ethanol/0.9% saline at 100 °C, using stannous chloride as the reducing agent. A study of the reaction parameters enabled the yield to be optimized to better than 90%, although this was reduced to approximately 60% if a purification step was carried out. Chromatographic analysis on ITLC-SG medium showed the final product to be of high radiochemical purity. Biological studies comprising biodistribution in mice over a 2-h period, imaging studies in animals and sub-acute toxicity testing in mice indicated that 99mTc-TBI prepared as here described is a suitable agent for routine clinical use in humans.

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