Compound Receptor selectivity Indication or use (phase)
Agonists    
Adenosine (Adenocard, Adenoscan) A1, A2A Paroxysmal supraventricular tachycardia (approved), myocardial perfusion imaging (approved), other uses in testing
Apadenoson A2A Myocardial perfusion imaging (III)
Regadenoson A2A Myocardial perfusion imaging (completed)
BAY 60-6583 A2B Atherosclerosis (preclinical)
Binodenoson A2A Myocardial perfusion imaging (III)
BVT.115959 A2A Diabetic neuropathic pain (II)
Capadenoson A1 Atrial fibrillation, chronic treatment (II)
LASSBio-1027 A2A/A3 Systemic hypertension (preclinical)
LASSBio-1386 A2A Pulmonary hypertension (preclinical)
LASSBio-1359 A2A Pulmonary hypertension (preclinical)
LASSBio-1366 A2A Pulmonary hypertension (preclinical)
MRS3558 A3 Autoimmune inflammatory diseases (preclinical)
Cl-IB-MECA A3 Liver cancer (I-II)
CP608,039 A3 Cardiac ischemia (discontinued)
Antagonists    
Caffeine A1/A2A/A2B/A3 Motor manifestations of Parkinson’s disease and excessive daytime somnolence in Parkinson’s disease (completed)
ATL 844 A2B Asthma and/or diabetes (preclinical)
Naxifylline A1 Heart failure (renal function) (discontinued)
FK-453 A1 Acute renal failure (preclinical)
Rolofylline A1 Heart failure (renal function) (discontinued)
Toponafylline A1 Heart failure (renal function) (IIb)
Vipadenant A2A Parkinson’s disease (II)
Table 2: Therapeutic use for agonists and antagonists of adenosine receptors. [16, 87,114, 118-120].