| DB00201 | Caffeine | approved | yes | antagonist | Details |
| DB04853 | Binodenoson | investigational | unknown | | Details |
| DB04932 | Defibrotide | approved, investigational | unknown | | Details |
| DB05191 | Atl146e | investigational | unknown | | Details |
| DB05009 | Apadenoson | investigational | unknown | | Details |
| DB00277 | Theophylline | approved | yes | antagonist | Details |
| DB06213 | Regadenoson | approved, investigational | yes | agonist | Details |
| DB00358 | Mefloquine | approved, investigational | unknown | antagonist | Details |
| DB00640 | Adenosine | approved, investigational | yes | agonist | Details |
| DB08770 | 4-{2-[(7-amino-2-furan-2-yl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)amino]ethyl}phenol | experimental | unknown | | Details |
| DB00806 | Pentoxifylline | approved, investigational | yes | agonist | 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 |
| DB09273 | Doxofylline | experimental | unknown | antagonist | Details |
| DB00555 | Lamotrigine | approved, investigational | unknown | inhibitor | Details |
| DB14132 | 8-chlorotheophylline | experimental | yes | antagonist | Details |
| DB11757 | Istradefylline | approved, investigational | yes | antagonist | Details |
| DB17080 | KW-6356 | experimental | yes | antagonist | Details |
| DB00683 | Midazolam | approved, illicit | unknown | potentiator | Details |