adenosine receptor

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

Adenosine receptor antagonist 4 is an adenosine receptor antagonist.

Adenosine A1 receptor activator T62 is an allosteric enhancer of the adenosine A1 receptor, producing antinociception in animal models of acute pain and reducing hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR), exhibiting exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties, holding great promise for investigating cancer and neurodegenerative diseases [1].

Adenosine receptor antagonist 3 has the potential for cancer disease research which is a potent adenosine receptor antagonist [1].

Adenosine receptor inhibitor 2 (compound 14b) is a potent inhibitor of AR (adenosine receptor), exhibiting dual affinity towards A1 A2A ARs with higher affinity for A1- than A2A AR, and Ki values of 52.2 nM for A1 AR and 167 nM for A2A AR.

Adenosine receptor antagonist 2 is an orally active A2a (IC50: 1 nM) and A2b (IC50: 3 nM) adenosine receptor antagonist with antitumor properties.

Adenosine receptor antagonist 1 is a highly selective A2aR adenosine receptor antagonist with an IC50 value of 0.29 nM and shows a 14-fold greater selectivity for A2aR over A2bR.

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

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.

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.

Adenosine monophosphate (AMP) is a purine ribonucleoside 5'-monophosphates and a key cellular metabolite in signal transduction and regulation of energy homeostasis.It has a role as an EC 3.1.3.11 (fructose-bisphosphatase) inhibitor, an EC 3.1.3.1 (alkaline phosphatase) inhibitor and an adenosine A1 receptor agonist.

Proxyphylline (7-(2-Hydroxypropyl)theophylline) is a dual of adenosine A1/A2a receptor inhibitor and phosphodiesterase (PDE) inhibitor. Proxyphylline acts as a cardiac stimulant, vasodilator and bronchodilator.

Ticlopidine hydrochloride (Ticlodix) is an effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.

Acefylline (Theophylline-7-acetic acid), a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the pharmaceutical preparation Etanautine to help offset its stimulant effects

Adenine monohydrochloride hemihydrate is a high affinity adenine receptor agonist (Ki = 18 nM at rat adenine receptor). It inhibits forskolin-stimulated cAMP formation in CHO cells transfected with the adenine receptor and also stimulates GTPγS binding (pEC50 values are 8.54 and 7.21 respectively).

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.

Theophylline (1,3-Dimethylxanthine) is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac, and central nervous system stimulant activities. It inhibits the 3', 5'-cyclic nucleotide phosphodiesterase that degrades cyclic AMP, thus potentiating the actions of agents that act through adenylyl cyclases and cyclic AMP.

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.

Aminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor giving a bronchodilatory effect.

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.

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.

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

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.

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

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.

SDZ WAG 994 is an A1 adenosine receptor agonist.

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

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.

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

RWJ-51204 is a selective adenosine A2A receptor antagonist and a partial agonist of GABA(A) receptor (IC50: 0.2-2 nM). It has neuroprotective and movement-improving effects and can be used in research related to Parkinson's disease.

CHEMBL241987 targets the Adenosine receptor A3 (human)

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.

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).

Pyrazolo[1,5-a]pyrimidine 4h is a morpholine derivative that is a selective antagonist of the adenosine A2A receptor. It has been shown to be neuroprotective in animal models of Parkinson's disease and Huntington's chorea.

A2B receptor antagonist 2 hydrochloride is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

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

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.

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

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.

A2A receptor antagonist 1 (CPI-444 analog) is an inhibitor of the adenosine A2A receptor and A1 receptor with Ki values of 4 nM and 264 nM, respectively.

GW-328267 is an agonist of the adenosine A2 receptor.

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

MRS 1754 is a selective antagonist radioligand for the A2B adenosine receptor, exhibiting very low affinity for A1 and A3 receptors in both humans and rats.

FPMPA PM is a derivative of FPMPA, a selective adenosine A3 receptor agonist with anti-inflammatory, analgesic and neuroprotective activities.

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

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.