Synthesis and biodistribution of radioiodinated‐5‐iodonicotine

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Abstract
5‐Bromonicotine, synthesized from nicotinic acid, was autoclaved with Na125I in the presence of copper sulfate and glacial acetic acid to give 5‐[125I]iodonicotine. The radiochemical yield was 25.3%. The specific activity of the product was approximately 61 mCi/mmole. Biodistribution studies of 5‐[125I]iodonicotine, performed in rats, showed that the labelled compound accummulated rapidly in the brain and the adrenal gland. The highest uptake of radioactivity in these organs occurred at 5 minutes after administration. The brain‐to‐blood and the adrenal‐to‐blood ratios at this time interval were 2.6:1 and 3.3:1 respectively.