Design, Synthesis, and Evaluation of New Organomedicinal Radiopharmaceuticals. Progress Report, March 1, 1981-February 28, 1982

摘要

The goal of this project is the development of radiopharmaceuticals which localize selectively in the normal myocardium and which can be used to assess myocardial perfusion and function with external detection systems. The availability of T1-201 as a myocardial imaging agent makes it possible to visualize compromised myocardium as an area of decreased radionuclide uptake. However, the long physical and biologic half-lives of this nuclide, as well as the low energy of its gamma emission and its cost, suggest a need to develop radiodiagnostic agents which have a similar myocardial distribution but employ a less expensive radioisotope with better decay properties. An approach developed in this proposal involves the use of cardioselective sympatholytic agents into which a suitable radionuclide can be incorporated. The two types of compounds to be investigated are the beta adrenoceptor antagonists and the catecholamine depleting agents. The radiolabeled products will be evaluated in normal and in experimentally infarcted animals, and their pharmacokinetics compared with those of T1-201. The most promising radiopharmaceuticals will subsequently be tested in larger animals having myocardial pathology.