A2a--Adenosine Agonist for Cardiovascular Imaging

Adenosine produces coronary vasodilation through activation of A-2a adenosine receptors. However adalso acts at A1 adenosine receptors to slow atrioventricular conduction and when injected into man ican be blocked with A1 receptor antagonists. DTI has synthesized a number of adenosine analogs that2a subtype of adenosine receptor and have identified WRC-0470 as a potent selective short acting corour belief that WRC- 0470 will prove to be superior to currently available pharmacological stress agbe a useful diagnostic aid in myocardial imaging techniques. We will i) develop synthetic chemical pefficient scale up of bulk material, ii) determine the stability of the compound in a variety of solvehicle for use as an injectable drug, iii) determine the safety and the optimal mode of administratconscious dog model in which coronary vasodilation and other cardiovascular parameters may be measurPhase II will support manufacture of clinical trials supplies, toxicology, and Phase I and Phase II