adenosine receptor

Adenosine receptor antagonist 4 is an 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.

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.

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

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

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.

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.

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

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.

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.

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.

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.

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.

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

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.

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

ANR94 is a potent, selective antagonist of the adenosine A2A receptor (AA2AR), exhibiting a K_i value of 46 nM for the human AA2AR (hAA2AR). This compound shows promise for research into Parkinson's disease. [1] [2]

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.

MRS-3777 hemioxalate, a selective adenosine A3 receptor antagonist, reverses the anti-injury perception effects of its corresponding agonist and serves as a valuable tool for studying inflammatory pain.

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.

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

A2AR-antagonist-1 (compound 38), an orally active adenosine A2A receptor antagonist with an IC50 value of 29 nM, demonstrates anti-tumor properties and stability in mouse liver microsomes (t1 2 = 86.1 min). Additionally, it activates T cells by inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and promoting expression of effector molecules (GZMB, IFNG, and IL-2) [1].

PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist, with K i values of 44.4 nM for rat A2A receptors and 360 nM for human A2A receptors. For rat and human A1 receptors, it has significantly lower affinity, with K i values of ≥10000 nM and 541 nM, respectively. The compound exhibits poor brain penetration and is not orally absorbable. It is of interest in research related to inflammatory bowel disease (IBD) [1] [2] [3].

A1 A3 AR Antagonist 3 is a dual A1R A3R antagonist that demonstrates high affinity within the low-micromolar to nanomolar range, and is potentially useful in the research of chronic heart diseases [1].