Adenosine Receptor

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.

Theobromine (3,7-Dimethylxanthine), a xanthine alkaloid, is used as a bronchodilator and as a vasodilator.

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.

Doxofylline (Doxophylline) is a methylxanthine derivative with the presence of a dioxolane group in position 7. As a drug used in the treatment of asthma, doxofylline has shown similar efficacy to theophylline but with significantly fewer side effects in animal and human studies.

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.

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.

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

Xanthine amine congener trihydrochloride is a potent adenosine antagonist that reverses the reduction in urine flow, sodium excretion and heart rate produced by the adenosine agonist, N6-cyclohexyladenosine.

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.

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

1-Ethyl-6-aminouracil (6-AMINO-1-ETHYL-1H-PYRIMIDINE-2,4-DIONE) is an intermediate in the synthesis of a series of new substituted Xanthines which have high affinity and selectivity for the human adenosine A2B receptors.

ISAM-140 is a potent and highly selective antagonist of A2B adenosine receptor.

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.

Apadenoson TFA is a potent adenosine A2A receptor (A2AR) agonist that can be used to improve survival in patients infected with SARS.

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.

LAS38096 is an A2B adenosine receptor antagonist (Ki : 17 nM) that is potent, selective and efficient .

Sulmazole (AR-L 115-BS) is a small molecule Sulmazole is a small molecule cGMP-PDE inhibitor.Sulmazole is a competitive inhibitor of A1 adenosine receptors.Sulmazole has been shown to improve cardiac index, low pulmonary capillary wedge pressure, and can be used in the study of heart failure.Sulmazole is a small molecule cGMP-PDE inhibitor.

Selodenoson (RG-14202) is a selective adenosine A1 receptor agonist used to slow the heart rate in patients with atrial fibrillation and to treat arrhythmias.

SDZ WAG 994 is an A1 adenosine receptor agonist.

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

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

GS-9667, a selective and partial agonist of the A(1) adenosine receptor (AR), represents an effective therapy for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA).

Sonedenoson (MRE0094) is an adenosine A(2A) receptor agonist and potential inhibitor potentially targeting SARS-CoV-2 coronavirus 2;-O-ribose methyltransferase, and may be used in the study of diabetic foot ulcers.

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

CHEMBL241987 targets the Adenosine receptor A3 (human)

KFM19 is a potent and selective adenosine receptor (A1-receptor) antagonist (IC50 : 50 nM) for the study of neurological disorders.

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.

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

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.

GS-6201 (CVT-6883) is a selective antagonist of adenosine A2B receptor. GS-6201 shows high affinity and selectivity for the human adenosine A2B receptors with a Ki of 22 nM.

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.

human A2B adenosine receptor antagonist

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.

N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine) is an adenosine derivative and an agonist of adenosine receptors with Ki values of 11.8 nM and 30.1 nM for rat and human A1.

MRS 1754 is a selective antagonist radioligand for the A2B adenosine receptor. It has a very low affinity for A1 and A3 receptors of both humans and rats.

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.

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.CAS 번호13483-88-88-9

Diphylline (Diprophylline) is a xanthine derivative. Diphylline exerts bronchodilator effects and to a lesser extent vasodilator and diuretic properties. Diphylline probably acts as a competitive inhibitor of phosphodiesterase which leads to an increase in intracellular cAMP. This results in relaxation of bronchial smooth muscle and other smooth muscles. Diphylline may also antagonize adenosinereceptors. Diphylline is used in the treatment of acute bronchial asthma, chronic bronchitis and emphysema.

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.

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

DPCPX (PD 116948) is an A1 adenosine receptor antagonist

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

CCPA (2-chloro-N(6)cyclopentyladenosine) is a potent and selective agonist of adenosine A1 receptor

Xanthine (Isoxanthine) is a product on the pathway of purine degradation. Xanthine is subsequently converted to uric acid by the action of the Xanthine oxidase enzyme. Xanthine is found in most body tissues and fluids in various organisms. Biologically Xanthine is produced from guanine by cypin (guanine deaminase). Furthermore, Xanthines act as antagonists for adenosine receptors, with selectivity depending on whether there are substitution of alkyl groups.

8-Cyclopentyl-1,3-dimethylxanthine (CPT) is a potent antagonist of adenosine A1 receptor.

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

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

SCH 58261 is a potent and selective A2a adenosine receptor antagonist.The Ki =2.3 nM for rat A2a and 2 nM is for bovine A2a.

Adenosine 5'-monophosphate monohydrate (5'-AMP) , also known as 5'-adenylic acid, is a nucleotide that is used as a monomer in RNA. It is an ester of phosphoric acid and the nucleoside adenosine. Adenosine 5'-monophosphate monohydrate consists of a phosphate group, the sugar ribose, and the nucleobase adenine. As a substituent it takes the form of the prefix adenylyl-.

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