| DB00201 | Caffeine | approved | yes | antagonist | Details |
| DB00996 | Gabapentin | approved, investigational | unknown | agonist | Details |
| DB04954 | Tecadenoson | investigational | unknown | | Details |
| DB04932 | Defibrotide | approved, investigational | unknown | | Details |
| DB12670 | Rolofylline | investigational | unknown | | Details |
| DB01223 | Aminophylline | approved | yes | antagonist | Details |
| DB00277 | Theophylline | approved | yes | antagonist | Details |
| DB12569 | Tonapofylline | investigational | unknown | | Details |
| DB00640 | Adenosine | approved, investigational | yes | agonist | Details |
| DB00806 | Pentoxifylline | approved, investigational | unknown | | Details |
| DB00651 | Dyphylline | approved | yes | antagonist | Details |
| DB01303 | Oxtriphylline | approved | yes | antagonist | Details |
| DB01412 | Theobromine | investigational | yes | antagonist | Details |
| DB00824 | Enprofylline | approved, experimental | unknown | inhibitor | Details |
| DB06471 | Naxifylline | investigational | unknown | antagonist | Details |
| DB00555 | Lamotrigine | approved, investigational | unknown | inhibitor | Details |
| DB09061 | Cannabidiol | approved, investigational | unknown | activator | Details |
| DB00193 | Tramadol | approved, investigational | yes | agonist | Details |
| DB11757 | Istradefylline | approved, investigational | no | antagonist | Details |