Table 2.
Molecules presented here that target adenosine receptors. None are approved for treatment
| Name | Target | Clinical use |
|---|---|---|
| Adenosine receptor agonists | ||
| GR79236 | Highly potent and selective adenosine A1 receptor agonist [12] | Ischemic heart disease [3, 25], sleep apnea [5], modulation of lipolysis and insulin sensitivity [18] |
| GR79236X | Selective adenosine A1 receptor agonist [6] | Ischemic heart disease [44] and dental pain [41] |
| GR190178 | Low efficacy (partial) adenosine A1 receptor agonist [13] | Cluster headache [13] |
| CGS21680 | Selective adenosine A2A receptor agonist [6] | Huntington’s disease [7], spinal cord injury [36], bone regeneration [33] and overactive bladder [47] |
| 2-CI-IB-MECA | Selective adenosine A3 receptor agonist [6] | Atrial function [49], damage of the optic nerve and white matter ischemic damage [14] |
| Adenosine receptor antagonists | ||
| Caffeine | Non-selective adenosine A1 and A2A antagonist [34] | Treatment of headache, pain, apnea in premature children and neurodegenerative diseases [10] |
| DPCPX | Selective adenosine A1 receptor antagonist [6, 13] | Depression [42], cancer [8, 30, 50] and neuroprotection [37] |
| SCH58261 | Potent and highly selective A2A receptor antagonist [15] | Spinal cord injury [36], epilepsy [29] and preeclampsia [40] |
| JNJ-41942914, JNJ-39928122, JNJ-40529749, JNJ-40064440, and JNJ-41501798 | A2A receptor antagonists [16] | None |