Xanthine amine congener is a non-selective adenosine receptor antagonist[1]. Xanthine amine congener induces convulsions in mice[2].
Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model[1].
SDZ-WAG994 (WAG-994) is a stable, long-acting, selective and orally active A1-adenosine receptor agonist with a KD of 23 nM. SDZ-WAG994 can be used for the research of atrial fibrillation[1].
Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.
5'-(N-Cyclopropyl)carboxamidoadenosine (CPCA) is an adenosine A2 receptor agonist[1].
PQ-69 is a potent and selective adenosine A1 receptor antagonist with inverse agonist activity. PQ-69 binds to hA1 receptor with a Ki value of 0.96 nM, is 217-fold more selective compared with hA2A receptors (Ki=208 nM) and >1,000-fold selectivity over hA3 receptor (Ki >100 μM). PQ-69 can be used for the research of renal dysfunction[1].
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[1].
Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
LASSBio-1359 is an adenosine receptor agonist. It acts by inducing relaxation of the corpus cavernosum. It also acts as a novel selective phosphodiesterase.
MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats[1].
Namodenoson (CF-102) is a selective A3 adenosine receptor agonist (Ki = 0.33 nM). Displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
PSB-12379 is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).
PSB-603 is a potent and selective adenosine A2B receptor antagonist exhibiting a Ki value of 0.553 nM at the human A2B receptor and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM[1].
Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].
A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively[1].
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes[1][2][3].
A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases[1].
KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively[1][2].
Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
CD73-IN-1 is an inhibitor of CD73 which can be used in the treatment of cancer extracted from patent WO 2017153952 A1, example 80.
A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations[1].
ISAM-140 (22b) is a potent and highly selective A2B adenosine receptor antagonist with a Ki of 3.49 nM[1].
Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
5'-N-Ethylcarboxamidoadenosine (NECA) is a nonselective adenosine receptor agonist.
MRS-1706 is a potent and selective A(2B) adenosine receptor antagonist with a Ki value of 1.39 nM.
Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis[1][2].
A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor[1].
A1AR antagonist 5 (compound 20) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.83 and a pKi of 6.11[1].
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM)[1]. GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse[2]. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice[3].
MRE3008F20 is a highly potent and selective antagonistic of adenosine A3 receptor (AA3R), inhibits agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM[1].