Table 1.
Therapeutic indications for selective A1 and A3 adenosine receptor ligands
| Adenosine receptor | Changes following genetic deficit or overexpression | Potential therapeutic indications | Example drugs | |
|---|---|---|---|---|
| A1 | Analgesic effects of adenosine abolished in A1-KO mice. Overexpression of cardiac A1 receptors caused increased resistance to ischaemia. | Agonist | Atrial fibrillation, angina, hyperlipidaemia, neuropathic pain, paroxysmal supraventricular tachycardia, cardiac ischaemia | Capadenoson, Tecadenoson, RPR749, GR79236 |
| Antagonist | Acute renal failure, heart failure (renal function) | FK-453, SLC320 | ||
| A3 | Enhanced antigen-stimulated mast cell degranulation by A3-agonists lost in A3-KO mice. Studies with congenic A3-/- mice indicate a cadioprotective effect of A3-receptor activation. | Agonist | Liver cancer, rheumatoid arthritis, autoimmune inflammatory disease, dry eye, cardiac ischaemia, dry eye | Cl-IB-MECA (CF102) MRS3558 (CF502) IB-MECA (CF101) |
| Antagonist | Asthma, glaucoma | KF26777, OT-7999 | ||
KO, knockout.