PREPARATION AND EVALUATION OF SOME ANTIARRHYTHMIC AND CARDIAC INOTROPIC AGENTS AS COLD ANALOGS OF POTENTIAL MYOCARDIAL IMAGING AGENTS

The iodinated anti-arrhythmic analogs of disopyramide (1), procainamid e (2) and lidocaine (3) and a new class of imidazolone cardiac inotrop ic dies inhibitors (4) and (5) (enoximone analogs), were prepared and tested as potential myocardial imaging agents. Compounds 1 and 2 were prepared by direct iodination using iodine monochloride in acetic acid , while 3-5 were prepared from suitable starting materials. The tissue load of the iodinated compounds was determined, in rats, on the basis of their iodine content using adaptation of a recent modification of Sandell and Kolthoff assay. The biodistribution of I-125-iodo derivati ves of 2 and 4 were performed in mice. A pharmacokinetic study was per formed using 5 to determine the optimal time of Imaging post-injection . These compounds have shown significant localization in the heart tis sue.