L-Adenosine is a metabolically stable enantiomeric analog and also is a potential probe. L-Adenosine has weakly inhibitory adenosine deaminase (ADA) activity with an Ki value of 385 μM. L-Adenosine can be used for the research of adenosine uptake and accumulation.

M1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.

VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain.

Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline sodium glycinate inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline sodium glycinate induces apoptosis. Theophylline sodium glycinate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.

PSB-0788 (compound 17), xanthine-8-yl-benzenesulfonamide derivative, is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 (compound 17) can be used for the research for chronic inflammatory lung diseases.

LJ-4517 is a potent A2AAR antagonist, with a Ki of 18.3 nM. LJ-4517 is potent in displacing the binding of [3H]ZM241385 at WT A2AAR.

Xanthine amine congener (XAC) hydrochloride is a non-selective adenosine receptor antagonist. Xanthine amine congener hydrochloride induces convulsions in mice.

(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research.

hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research.

ATL-801, an A2B receptor selective antagonist, ameliorates murine colitis.

Inupadenant (EOS-850, EOS100850) is a non brain-penetrant, potent and highly selective small molecule antagonist of adenosine A2a receptor (A2AR), shows activity at the high adenosine concentrations found in tumors.

A1AR antagonist 1 (compound 18g) is a potent A1 adenosine receptor (AR) antagonist with Kis of 2.08, 6.91, and 31.2 nM for hA1, hA2A and hA2B, respectively.

PSB36 is a potent and selective antagonist of adenosine A1 receptor, with Kis 0.12 nM, 187 nM, 552 nM, 2300 nM, and 6500 nM for rA1, hA2B, rA2A, hA3 and rA3 receptors respectively. PSB36 can be used for the research of hyperalgesia.

VUF-5574 is a selective antagonist of adenosine A3 receptor with a Ki of 4.03 nM for the recombinant human receptor.

Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity.

A2A/A1 AR antagonist-1 (compound 1a) is dual potent A2A/A1 AR antagonist with Kis of 5.58 and 24.2 nM, respectively. A2A/A1 AR antagonist-1 has the potential for the research of ischemic stroke.

IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.

Adenosine receptor antagonist 3 is a potent antagonist of adenosine receptor. Adenosine receptor antagonist 3 has the potential for the research of cancer disease (extracted from patent WO2019233994A1, compound 1).

MRS1334 is a potent and selective human adenosine A3 receptor antagonist with Kis of 2.69 nM, >100 nM, >100 nM for hA3, rA1, rA2A, respectively. MRS1334 blocks the protective effect of Cl-IB-MECA leading to significant bradycardia and elevated ST segment.

A1AR antagonist 2 (compound 18h) is a potent A1 adenosine receptor (AR) antagonist with Kis of 1.49, 10.2, and 50.1 nM for hA1, hA2A and hA2B, respectively.

Heterobivalent ligand-1 (compound 26) is a heterobivalent ligand for the Adenosine A 2A-dopamine D 2 receptor heteromer (KDB1 A2AR=2.1 nM, KDB1 D2R= 0.13 nM).

Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier.

AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.

N6-Benzyl-5'-ethylcarboxamido adenosine is a selective A3 adenosine receptor agonist.

hA3AR agonist 1 is a potent human A3 adenosine receptor (hA3AR) agonist with a Ki value of 2.40 nM.

Adenosine receptor antagonist 1 is a A2aR-selective antagonist with an IC50 of 0.29 nM and displays 14-fold more selective for A2aRthan A2bR.

Binodenoson (MRE-0470) is a potent and selective A2A adenosine receptor agonist (KD=270 nM). Binodenoson is being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging.

UK-432097 is a highly potent and selective A2AAR agonist with a pKi of 8.4 for human A2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research.

A2B receptor antagonist 2 (compound 18) is an adenosine receptor A2B antagonist, with Ki values of 2.30 μM, 6.8 μM and 3.44 μM for rA1, rA2A and hA2B, respectively.

PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice.