-
Adenosine receptor antagonist
Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole. -
Adenosine receptor antagonist
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. -
A2A antagonist
Istradefylline (KW-6002) is a selective antagonist at the A2A receptor. It has been found to be useful in the treatment of Parkinson's disease.- PU Hamor, .et al. , Prog Neuropsychopharmacol Biol Psychiatry, 2020, Dec 20;103:109979 PMID: 32470496
-
A2a receptor antagonist
SYN115 is an orally administered, potent and selective inhibitor of the adenosine 2a (A2a) receptor that is being developed initially for the treatment of Parkinson?€?s disease, but may also have utility in other CNS disorders. -
Adenosine A2A Receptor Agonist
CGS 21680 is a specific adenosine A2A subtype receptor agonist.- Qian Wang, .et al. , Neuropharmacology, 2019, 148: 229-243 PMID: 30659840
-
A2A adenosine agonist
Regadenoson was selective agonist for the A2A adenosine receptor versus the A1, A2B, and A3 receptors in binding and functional studies. Regadenoson was also found to be a full and potent agonist to cause coronary vasodilation, a response that has a very large A2A receptor reserve? -
adenosine A2A/A1 receptor antagonist
A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively. -
Adenosine receptor inhibitor
N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5??-Nucleotidase. IC50 value: 29.0 ± 1.7 nM (Ki) Target: Adenosine Receptor -
A2A Receptor Antagonist
SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM). - Tamsulosin hydrochloride is an antagonist of alpha1A adrenoceptors in the prostate.
-
human A3 adenosine receptor antagonist /Aurora inhibitor
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.- Amy H. Ide, .et al. , Mol Biol Cell, 2023, Jun 1;34(7):ar76 PMID: 37126397
- Hazheen K, .et al. , J Biol Chem, 2020, August 20
-
A1 adenosine receptor agonist
Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist. -
Adenosine A2A receptor antagonist
Preladenant is a potent and selective antagonist at the adenosine A2A receptor. -
Adenosine A2A antagonist
ZM-241385 is a potent and highly selective Adenosine A2A-R antagonist, with a pA2 of 9.02 for Adenosine A2A-R in cardiac vasculature and selectivities of 1000, 91 and 500,000 over Adenosine A1-R, Adenosine A2B-R and Adenosine A3-R sites, respectively.- Sheng-Tao Hou, .et al. , Research Square, 2023, Sep 28
-
human 5'-methylthioadenosine phosphorylase inhibitor
MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM. -
adenosine A2B receptors antagonist
CVT-6883, a selective A2B adenosine antagonist, represents a novel potential approach to treating cardiopulmonary diseases. -
Adenosine kinase inhibitor
5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM.- Jing-Yu Lin, .et al. , Cell Discov, 2020, 6: 20 PMID: 32284878
-
A2A receptor antagonist
Vipadenant, also known as BIIB014, CEB-4520, is a potent, selective and orally available adenosine A2A receptor antagonist under development for Parkinson's disease. Vipadenant demonstrates strong oral activity in commonly used models of Parkinson's disease. -
Adenosine Receptor agonist
Capadenoson is a selective agonist of adenosine-A1 receptor. -
Adenosine A3-R agonist
IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nM for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively.- Sameshima T, .et al. , Chem Res Toxicol, 2019, Aug 28 PMID: 31461269
-
Adenosine A3 receptor agonist
CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. -
Adenosine A Receptor agonist
2-Chloroadenosine is a metabolically stable analog of adenosine that behaves as an Adenosine A Receptor agonist (Ki values are 300, 80 and 1900 nM for Adenosine A1-R, Adenosine A2A-R and Adenosine A3-R, respectively). -
Adenosine A2 receptor agonist
CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor. -
A2 receptor antagonist
Alloxazine is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor. -
A2AR antagonist
AZD-4635 (HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors. -
A1 adenosine receptors antagonist
Proxyphylline is a derivative of theophylline which is used as a bronchodilator and for its cardiovascular properties. It selectively antagonizes A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 μM for platelets). -
Adenosine receptor antagonist
Theophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class. -
Adenosine A1 receptor agonist
N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively. -
adenosine A3 receptor antagonist
MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibits agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM. -
Adenosine receptor agonist
N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively. -
A1 adenosine receptor agonist
N6-(2-Phenylethyl)adenosine is a selective A1 adenosine receptor agonist. -
adenosine receptor antagonist
Taminadenant is an antagonist of adenosine receptor. -
AA3R antagonist
Adenosine antagonist-1 is an adenosine A3 receptor (AA3R) antagonist. -
A1 receptor agonist
N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM).