Adenosine Receptor

A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

Fostamatinib (R788)(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.

CPI-444 (V81444) is an antagonist of the adenosine A2A receptor.It reduces tumor area in mouse model of murine Her2 neu-expressing breast cancer.

ABT-702 dihydrochloride is a highly potent inhibitor of adenosine kinase (AK).

MRE3008F20 is a species-selective and potent adenosine A3 receptor (AA3R) antagonist that inhibits Cl-IB-MECA-induced cAMP production and can be used in glaucoma and asthma studies.13483-88-88-9

AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR A2bR) antagonist. It has immunomodulatory activity[1].

Inosine (NSC-20262) is a purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It has immunomodulatory, neuroprotective, and analgesic properties.

Evodenoson (ATL313) is a potent and selective adenosine A2a receptor (A2aR) agonist for the treatment of eye diseases, tumors, and immune system disorders, and may be used in studies of open-angle glaucoma and blood tumors.

A2AR-agonist-1 (N-(2-(1H-Indol-3-yl)ethyl)adenosine) is a potent A2AR and ENT1 agonist (Ki: 4.39 and 3.47 for A2AR and ENT1. It targets the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.

AZD4635 (HTL1071) is a new-type adenosine 2A receptor (A2AR) inhibitor(Ki=1.7 nM).

Regadenoson (CVT-3146) is an adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selectively binds to and activates the A2A adenosine receptor, which induces coronary vasodilation. This leads to an increase in coronary blood flow and enhances myocardial perfusion. Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor. This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors.

YT 146 is a selective adenosine receptor A2 agonist with cardioprotective and vasodilatory effects that inhibits neointimal thickening after endothelial injury in rat femoral arteries.

5'-Amino-5'-deoxyadenosine (NH2dAdo) is an adenosine kinase inhibitor targeting malignant tumors of the inert lymphatic system with antitumor and anticancer effects. Its mechanism is mediated by the inhibition of DNA synthesis and induction of apoptosis.

CGS 21680 Hydrochloride (CGS 21680 HCl)(IC50=22 nM), an adenosine receptor agonist, exhibits 140-fold potency in A2 receptor over A1 receptor.

PSB-603 is a selective antagonist of Adenosine A2B receptor(Ki = 0.553 nM) with anti-inflammatory effects.

5'-N-Ethylcarboxamidoadenosine (NECA), an agonist of the Adenosine receptor, increases cerebral extravasation of fluorescein and low molecular weight dextran independent of blood-brain barrier modulation.

1. Norisoboldine ((+)-Laurelliptine) might be a potential therapeutic agent for rheumatoid arthritis, and it functions through protecting joint destruction as well as regulating the abnormal immune responses. 2. Norisoboldine inhibits the macrophage activation and the resultant production of pro-inflammatory cytokines via down-regulating the activation of MAPKs signaling pathways rather than NF-κB.

MRS1220, a selective and potent antagonist for the human A3 adenosine receptor (hA3AR) with a dissociation constant (Ki) of 0.59 nM, exhibits therapeutic promise for central nervous system disease research. It effectively diminishes glioblastoma tumor size and inhibits blood vessel formation in vivo.

5-Iodotubercidin (NSC-113939) is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.

Istradefylline (KW-6002)(Ki of 2.2 nM) is a selective adenosine A2A receptor (A2AR) antagonist, which is under development in Phase 3 trails. It has been used in trials studying the treatment and basic science of Drug Abuse, Sleep Disorder, Hepatic Impairment, Parkinson's Disease, and Restless Legs Syndrome, among others.

Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.

BAY 60-6583 is a potent, high-affinity adenosine A2B receptor agonist (EC50 = 3 nM) with affinity for A2B receptors that exceeds that for A1, A2A, and A3 receptors.BAY 60-6583 is cardioprotective in a model of myocardial ischemia.The Ki values for BAY 60-6583 binding to mouse, rabbit, and dog A2BAR were 750 nM, 340 nM, and 330 nM, respectively. The Ki values of BAY 60-6583 binding to A2BAR in mice, rabbits and dogs were 750 nM, 340 nM and 330 nM respectively.

Swertisin, a novel herbal biomolecule, shows a strong antihyperglycemic action. Swertisin is an adenosine A1 receptor antagonist, is known to have antidiabetic, anti-inflammatory and antioxidant effects.

FK-453 is a potent antagonist of non-xanthine adenosine A1 receptor with diuretic and renal vasodilatory activity.