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High Myocardial Accumulation of Radioiodinated Digoxin Derivative: A Possible Na, K-ATPase Imaging Agent

Faculty of Pharmaceutical Sciences and School of Medicine, Kyoto University, Kyoto, Japan

Correspondence: For reprints contact: Akira Yokoyama, PhD, Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Shimoadachi-cho, Yoshida, Sakyo-ku, Kyoto, 606, Japan.

ABSTRACT

In view of the high binding ability of cardiac glycosides to the myocardial Na,K-ATPase, radioiodinated digoxin derivatives were surveyed as candidates for myocardial imaging, with particular emphasis on the noninvasive monitoring of cardiac glycoside therapy. Among the radioiodinated digoxin derivatives surveyed, ¹²⁵I-digoxin-iodohistamine(bis(O-carboxymethyloxime)) showed the highest accumulation in the myocardium and similar binding ability to Na,K-ATPase as digoxin itself against ouabain displacement, as indicated by in vivo and in vitro studies. Based on these results, ¹²³I labeling of digoxin-histamine(bis(O-carboxymethyloxime)) and imaging in a dog demonstrated uptake in the myocardium.