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4-[¹²⁵I] Iodophenyltrimethylammonium Ion, an Iodinated Acetylcholinesterase Inhibitor with Potential as a Myocardial Imaging Agent

The Johns Hopkins University, Baltimore, Maryland

Correspondence: For reprints contact: H. Donald Burns, PhD, Div. of Nuclear Medicine, Johns Hopkins Medical Institutions, 615 N. Wolfe St., Baltimore, MD 21205.

ABSTRACT

4-[¹²⁵I]Iodophenyltrimethylammonium acetate (4-I-125 PTMA) was prepared by Chloramine-T iodination of N,N-dimethylaniline and subsequent methylation with methyliodide. Purification by thin layer chromatography afforded a product whose specific activity approached the theoretical carrier-free level.

Biodistribution studies in normal ICR mice showed a significant accumulation of 4-I-125 PTMA in the heart tissue, with heart-to-blood ratios of 12.5, 10.4, 7.8, 3.4, 3.4, and 3.3 at 1, 5, 10, 30, 60, and 120 min, respectively. Initial uptake in the heart was greater than 26% of the injected dose per gram. Twenty-five percent of the activity was excreted unchanged by the kidneys during the first 5 min. Less than half of the injected activity was retained in mice at 120 min.