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. Author manuscript; available in PMC: 2021 Jul 1.
Published in final edited form as: Pharmacol Ther. 2020 Mar 19;211:107529. doi: 10.1016/j.pharmthera.2020.107529

Table 2 —

Chemical compounds targeting adenosine receptors

Drug Pharmacological effects Clinical effects References Stage of development
AMP579 Agonist of A2B receptor Cardio-protection PMID: 19730798 Preclinical
Capadenoson (BAY 68-4986) Partial agonist of A1 receptor Anti-anginal PMID: 22370739 NCT00568945 Phase 1 trials
Derenofylline (SLV-320) Antagonist of A1 receptor Diuresis PMID: 21641345 NCT00744341 Phase 2 trials
FK-352 Antagonist of A1 receptor Improves intra-dialytic hypotension PMID: 16395260 Phase 2 trials
GS-9667 (CVT-3619) Partial agonist of A1 receptor Anti-insulin sensitizer PMID: hyperlipidemic, 23427000 PMID: 18494808 Phase 1 trials
MRS-5698 A3 receptor agonist Analgesia PMID: 26111639 Preclinical
Namodenoson (CF-102) A3 receptor agonist Antineoplastic PMID: 23299770 Phase 2 trials
Neladenoson Partial agonist of A1 receptor Cardio-protection PMID: 27624622 Phase 1 trials
PBF-509 Antagonist of A2A receptor Antineoplastic NCT02403193 Phase 2 trials
PBF-680 Antagonist of A1 receptor Bronchodilation NCT03774290 Phase 2 trials
PBF-999 Antagonist of A2A receptor Antineoplastic NCT03786484 Phase 1 trials
Piclidenoson (CF-101) A3 receptor agonist Immuno-modulatory NCT03168256 Phase 3 trials
Preladenant (SCH-420814 or MK-3814) Antagonist of A2A receptor Neuroprotection NCT01227265 Phase 3 trials
Rolofylline (KW-3902) Antagonist receptor of A1 Diuresis PMID: 20925544 Phase 3 trials
Selodenoson (RG-14202) Partial agonist of A1 receptor Coronary vasodilator PMID: 8496817 Preclinical
T-62 Partial agonist of A1 receptor Analgesia NCT00809679 Phase 2 trials
Tecadenoson (CVT-510) Partial agonist of A1 receptor AV node blockade PMID: 15956124 Phase 3 trials
Tonapofylline (BG-9928) Partial agonist of A1 receptor Diuresis PMID: 20926754 Phase 1 trials
Trabodenoson (INO-8875) Partial agonist of A1 receptor Reduces intra-ocular pressure PMID: 27046445 Phase 2 trials
V-81444 Antagonist of A2A receptor ADHD Parkinson’s disease NCT02253745 NCT02764892
VCP-746 Partial agonist of A1 and A2B receptors Cardio-protection PMID: 27377874 Preclinical
WRC-0571 Inverse agonist of A1 receptor Tachycardia PMID: 8632314 Preclinical

ADHD = Attention deficit-hyperactivity disorder; NCT = National ClinicalTrials.gov number; PMID = PubMed identifier.