2-Phenylaminoadenosine (CV-1808) is an adenosine A2 receptor agonist. CV-1808 is a coronary vasodilator, antihypertensive and antipsychotic following systemic administration in vivo. CV-1808 appeared to be effective for salvaging ischemic myocardium. The effect might be related to improvement of coronary circulation and inhibition of release of vasoactive substances, including TXA2, from the ischemic myocardium. Development of CV-1808 has been discontinued in the United States.

2-Fluoroadenosine (F-Ado) was developed at Southern Research Institute in 1957 as a potential anticancer drug. 2-Fluoroadenosine is not deaminated by adenosine deaminase but metabolized to triphosphate as shown in vitro. The drug was also shown to be a potent inhibitor of lymphocyte-mediated cytolysis.

GR79236 is an adenosine A1 receptor agonist, which possesses cardiovascular and antilipolytic properties. GR79236 was studied in model animals for the treatment of diabetic ketoacidosis and in patients for pain relief. However, these studies were discontinued. In addition, analgesic efficacy of GR79236 was investigated in the dental pain model. Nevertheless, there was no evidence of efficacy of GR79236. A higher dose of GR79236 might have been effective or that was suggested, that intravenous administration of that drug did not achieve appropriate concentrations in the brain or peripheral nerves.

SDZ-WAG-994 is a potent and selective A1 receptor agonist, discovered by Sandoz. SDZ-WAG-994 was able to induce a dose-related and sustained fall in blood pressure and heart rate in spontaneously hypertensive rats. The compound was investigated in patients with heart failure symptoms and moderate left ventricular systolic dysfunction, where it produced no effect. In patients with patients with permanent atrial fibrillation, SDZ-WAG-994 was able to limit the increase in mean heart rate during exercise. The compound was also tested for treatment of postoperative dental pain, but for all efficacy measures, SDZ-WAG-994 was not significantly different from placebo.