213594-73-1Relevant articles and documents
Preparation and evaluation of some anti-arrhythmic and cardiac inotropic agents as 'cold' analogs of potential myocardial imaging agents
El-Moselhy, Tarek F.,El-Kersh, Mohamed A.,Nyberg, Fred,Hede, Ragnar,Eldawy, Mohamed A.
, p. 163 - 170 (2007/10/03)
The iodinated anti-arrhythmic analogs of disopyramide (1), procainamide (2) and lidocaine (3) and a new class of imidazolone cardiac inotropic phosphodiesterase 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 125I-iodo derivatives of 2 and 4 were performed in mice. A pharmacokinetic study was performed using 5 to determine the optimal time of imaging post-injection. These compounds have shown significant localization in the heart tissue.