adenosine a3 receptor

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.

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.

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

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.

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.

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.

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.13483-88-88-9

Apadenoson is a potent Adenosine A2 receptor agonist with inhibitory effects on Adenosine A3 receptors with an IC of 45 nM. Apadenoson has anti-inflammatory activity and can be used to study neurological diseases.

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.

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

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

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

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

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.

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

N6-Cyclopentyladenosine (CPA) is a selective agonist of the adenosine A1 receptor, mimicking its action with Ki values of 2.3 nM, 790 nM, and 43 nM for human A1, A2A, and A3 receptors, respectively. CPA is used to modulate cellular signaling, neurotransmission, and other biological processes.

CHEMBL241987 targets the Adenosine receptor A3 (human)

LJ-2698 is an adenosine A3 receptor antagonist under investigation for treating emphysema and DKD (Diabetic Kidney Disease). In mouse lung models, LJ-2698 effectively mitigates elastase-induced adverse effects and inhibits matrix metalloproteinase activity and apoptosis. Additionally, it is being explored for its potential in treating diabetic nephropathy, successfully preventing various types of kidney damage in mice.

HEMADO is a potent and selective agonist of the adenosine A3 receptor [Ki: 1.1 nM at the human A3 subtype].

CELT-327 is a potent, selective fluorescent hA2B/A3 adenosine receptor antagonist, exhibiting K_i values of 35.6 nM at A2B and 45.7 nM at A3 receptors. It efficiently labels HCT116 cells expressing A2B adenosine receptors in a dose-dependent manner, demonstrating rapid, uniform spread and integration of fluorescence within cell monolayers. In live HCT116 spheroids, it achieves consistent staining throughout, penetrating even the deepest layers. As a fluorescent adenosine receptor probe, CELT-327 is ideal for applications in fluorescence binding assays, live cell imaging, flow cytometry, and fluorescence polarization assays, serving as an effective alternative to GPCR radiolabeling ligands. Its excitation and emission peaks are at 589 nm and 616 nm, respectively, making it suitable for TR-FRET assays as an acceptor dye, particularly in combination with the CoraFlor1 TR-FRET donor.

MRS8247 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR), which also slows the dissociation rate of the agonist.

MRS5698 is a high affinity and selective agonist of A3 adenosine receptor (Ki ~ 3 nM) protects against chronic neuropathic pain. MRS5698 displays >1000-fold selectivity over A1 and A2A adenosine receptors

MRS1067 is an antagonist of A3 adenosine receptor.