adenosinereceptor

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.

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

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.

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.

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

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.

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.

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.

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.

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]

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.

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].

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].

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].

Compound 19, a selective A3 Adenosine Receptor (A3AR) agonist (K i : 22.1 nM), effectively stimulates β-arrestin2 recruitment with an EC 50 value of 4.36 nM. This compound is utilized in research pertaining to inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions [1].

A3AR Agonist 1 (Compound 12), with a Ki of 25.8 nM, is a potent A3 adenosine receptor (A3AR) agonist that promotes β-arrestin2 recruitment with an effective concentration (EC50) of 5.17 nM. It serves as a research tool in various pathological conditions, including inflammatory diseases, ischemia, cancer, neuropathic pain, and liver diseases [1].

Derenofylline is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM)

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.

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.

Zaladenant is an adenosine receptor antagonist with antitumor properties.

8-Chloro caffeine binds to adenosine receptors with a Ki of 30 µM. It enhances UV-induced chromosomal aberrations in the Cl-I type Chinese hamster embryo lung cells. 8-Chloro caffeine is a derivative of the methylxanthine alkaloid caffeine.

ADORA2A PDE4D-IN-1 (Compound 9) is a dual inhibitor of the adenosine A2a receptor (ADORA2A) and phosphodiesterase 4D (PDE4D). This compound is applicable for research in bronchial asthma.