High myocardial accumulation of radioiodinated digoxin derivative: a possible Na,K-ATPase imaging agent. |
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Authors: | Y Fujibayashi Y Takemura K Matsumoto K Wada Y Yonekura J Konishi A Yokoyama |
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Institution: | Faculty of Pharmaceutical Sciences, Kyoto University, Japan. |
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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. |
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