Preladenant is a highly selective and competitive A2A receptor antagonist with Ki value of 1.1nM, used in trials studying the treatment of brain diseases, such as parkinson disease, movement disorders, antipsychotic agents and parkinsonian disorders.

N6-Cyclopentyladenosine is a potent and selective adenosine A1 receptor agonist with Ki of 2.3 nM for human A1 receptor.

SCH-442416 is a selective adenosine A2A receptor antagonist. SCH-442416 binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). It displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM).

CPI-444 is an orally administered antagonist of the adenosine A2A receptor. Upon oral administration, CPI-444 binds to adenosine A2A receptors expressed on the surface of immune cells, including T-lymphocytes, natural killer (NK) cells, macrophages and dendritic cells (DCs).

BAY 2416964 is an antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM.

VUF5574 is a potent, selective, competitive antagonist for the human adenosine A3 receptor with Ki of 4 nM.

Tecadenoson is a selective A1 adenosine receptor agonist.

Taminadenant is an antagonist of adenosine receptor.

2-Chloro-N6-cyclopentyladenosine is a potent and selective adenosine A1 receptor agonist with Ki of 0.8 nM for human A1.

CGS 15943 is a potent adenosine receptor antagonist with Ki values of 3.5, 4.2, 16 and 51 nM for human A1, A2A, A2B and A3 receptors respectively.

AZD4635 is an A2AR antagonist which can reverse adenosine mediated T cell suppression.

CVT-6883 is a selective antagonist of adenosine A2B receptors with Ki of 22 nM for human A2B.

AB928 is a dual A2aR/A2bR antagonist that inhibits A2aR and A2bR with an equilibrium binding constant of 1.4 and 2 nM, respectively.

N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM).

Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats[1].

N-[(4-Aminophenyl)methyl]adenosine is an adenosine receptor inhibitor, with Ki of 29 nM for rat ecto-5′-nucleotidase.

Capadenoson is an oral active, potent and selective adenosine A1 receptor agonist.

2-Cl-IB-MECA is a highly selective A3 adenosine receptor agonist with Ki value of 0.33nM, displaying 2500- and 1400-fold selectivity over A1 and A2A receptors, respectively.