Adenosine Receptor

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.

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

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

Amp579 TFA is a novel adenosine A1/A2a receptor agonist that induces acute and delayed preconditioning against myocardial shock in vivo.

Adenosine antagonist-1 acts as an adenosine A3 receptor (AA3R) antagonist.

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.

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.

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.

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

MIPS521 ({2-Amino-4-[3,5-bis(trifluoromethyl)phenyl]thiophen-3-yl}(4-chlorophenyl)methanone) is a positive allosteric modulator of the A1R.

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.

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.

Pentostatin (CI-825) is an extremely effective and irreversible inhibitor of adenosine deaminase (Ki: 2.5 pM).

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

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.

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.

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

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.

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.

CGS 15943 is an orally bioavailable non-xanthine antagonist of the Adenosine Receptor. In transfected CHO cells, its Ki values for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM, respectively.

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.

Tonapofylline is an orally active and selective antagonist of the A1 adenosine receptor (Ki: 7.4 nM for human A1). Tonapofylline can be used in studies about heart failure.

ZM-241385 is a high-affinity antagonist ligand selective for the adenosine A2A receptor.

Reversine, a small synthetic purine analogue (2, 6-disubstituted purine), is a potent inhibitior of Aurora A B C(IC50s=150-500 nM).

N 0861 is a selective adenosine A1 receptor antagonist that attenuates renal insufficiency during adenosine-controlled hypotension in rats.

DPTN dihydrochloride is a potent and selective A3AR antagonist with Ki values of 1.65, 9.61 and 8.53 nM in human, mouse and rat, respectively.

human A2B adenosine receptor antagonist

ST 1535 is a potent and orally active antagonist of the A2A adenosine receptor, exhibiting antiparkinsonian activity and antitremorigenic effects, with potential for Parkinson’s disease research.

Taminadenant is an adenosine receptor antagonist.

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

DPCPX (PD 116948) is an A1 adenosine receptor antagonist

Adenosine amine congener (ADAC) (ADAC) is an agonist of selective A1 adenosine receptor,.

Binodenoson (WRC 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].

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

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.

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.

Piclidenoson (CF-101), a selective agonist of adenosine A3 receptor(EC50 values of 0.11 μM), induces robust anti-inflammatory effect in psoriasis patients.

GW-493838 is a potent adenosine A1A receptor agonist for the treatment of dyslipidemia and neuropathic pain, with analgesic effects on post-herpetic neuralgia or peripheral nerve damage caused by trauma or surgery.

LUF6096 (CF-602) is a potent allosteric enhancer of the adenosine A3 receptor, exhibiting the capability to enhance agonist binding allosterically while demonstrating low orthosteric affinity across adenosine receptors. It displays protective effects in myocardial ischemia reperfusion injury.

7-Methylxanthine is a methyl derivative of xanthine, the purine component of human urinary calculi.7-Methylxanthine has an affinity for adenosine receptors.7-Methylxanthine is a methyl derivative of xanthine, the purine component of human urinary calculi.7-Methylxanthine has an affinity for adenosine receptors.

SDZ WAG 994 is an A1 adenosine receptor agonist.

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

Pentoxifylline (PTX) modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase and affects blood rheology. It also inhibits platelet aggregation and improves blood flow by increasing erythrocyte and leukocyte flexibility.

Quercetin-3'-o-phosphate TEA (Quercetin 3'-phosphate TEA) is an adenosine A receptor antagonist that can be used to prevent and treat metabolic disorders.

Nitrobenzylthioinosine (NBMPR) is an inhibitor of ENT1 transporter that binds to ENT1 transporter with high affinity.

Namodenoson (2-Cl-IB-MECA) is an adenosine A3 receptor agonist.

Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83) that blocks recall in fear conditioning in mice. It exhibits inverse agonist and antagonist activity (Ki, 220 nM) at the A2A receptor and weak antagonist activity (Ki, 736 nM) at the 5-HT2B receptor.