G-Protein Coupled Receptors and Cardiovascular Therapies

This article explains how G-protein coupled receptors are involved in many types of cardiovascular therapies. Adenosine, a purine nucleoside, activates four G-protein coupled receptors. There four receptors are A1, A2a, A2b, and A3. Activation of myocardial A1 receptors have been shown to inhibit a variety of myocardial pathologies associated with ischemia and reperfusion injury, These pathologies include stunning, arrhythmogenesis, coronary and ventricular dysfunction, acute myocardial infarction, apoptosis, and chronic heart failures. These findings imply several options for new cardiovascular therapies for diseases, like angina pectoris, control of cardiac rhythm, ischemic injury during an acute coronary syndrome, and heart failure.

 The main problem arising involving using full A1 agonists for these problems is the wide range of side effects. This is because of the broad physiologic spectrum of cardiac and extracardiac effects caused by the A1 receptor. This can be overcome by using partial A1 agonists. Partial A1 agonists can be used to trigger only some of the physiological responses of receptor activation. The responses triggered depend on the endogenous adenosine levels and on receptor reserves in different tissues.