adenosine antagonist-1

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

A2B receptor antagonist 1 is a small molecule antagonist and an A2B adenosine receptor antagonist with potent antagonistic activity, and can be used for research on adenosine receptor-related diseases.

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.

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.

L-97-1 is an antagonist of the adenosine A1 receptor.

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]

AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. It has immunomodulatory activity[1].

DMPX (3,7-Dimethyl-1-propargylxanthine) is a caffeine-like compound capable of crossing the blood-brain barrier. It serves as an A2-selective adenosine receptor (AR) antagonist, effectively and selectively blocking the hypothermia and behavioral inhibition induced by A2 adenosine receptor agonists, such as NECA. DMPX is utilized in research on diseases like Parkinson's disease.

A2AAR antagonist 4 is an orally active antagonist of the A2A adenosine receptor (A2AAR) with a Ki value of 0.36 nM and a KB value of 1 nM in humans. At a concentration of 10 μM, it fully inhibits both human A2AAR and human A2bAR. A2AAR antagonist 4 is applicable in cancer research, such as studies involving MC38 tumors.

BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM) that inhibits CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM). It is also efficacious in the Defensive Withdrawal model of anxiety in rats and has low in vivo clearance [Cl = 17 mL/min/kg, t½ = 7.8 h].

Inupadenant is an orally active, highly selective A2A receptor antagonist with potent anti-tumor activity [1] and is not brain-penetrant.

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.

Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor that targets PDE3 to relax airway smooth muscle and is used in asthma and chronic obstructive pulmonary disease (COPD) research. It also functions as an adenosine receptor antagonist, histone deacetylase (HDAC) activator, and exhibits anti-inflammatory activity by increasing IL-10 levels and inhibiting NF-κB nuclear import, while inducing apoptosis [1] [2] [3] [4] [5].

A1AR antagonist 2 (compound 18h) is a potent antagonist of the A1 adenosine receptor (AR) with Ki values of 1.49, 10.2, and 50.1 nM for hA1, hA2A, and hA2B, respectively [1].

A2AAR antagonist 1 (compound 21a) is a potent A2AAR (adenosine A2A receptor) antagonist with high ligand efficiency and a Ki value of 20 nM. It is applicable in neurodegenerative disease research [1].

A1AR antagonist 6 (compound 15) is a potent and selective inhibitor of the A1 adenosine receptor (A1AR), exhibiting a pKi of 7.13 and a pIC50 of 6.38[1].

A1AR antagonist 1 (compound 18g) is a potent A1 adenosine receptor (AR) antagonist with Ki values of 2.08, 6.91, and 31.2 nM for hA1, hA2A, and hA2B, respectively [1].

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

A1AR antagonist 5 (compound 20) is a potent and selective inhibitor of the A1 adenosine receptor (A1AR) with a pKi of 6.11 and a pIC50 of 5.83 [1].

A1AR antagonist 4 (compound 22) is a potent and selective A1 adenosine receptor (A1AR) antagonist with a pIC50 value of 5.51 and a pKi value of 6.29 [1].

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].

A1/A3 AR antagonist 1 (Compound 10) is a potent, dual adenosine 1 (A1) and adenosine 3 (A3) receptor antagonist that acts on human A1 (Ki: 37.6 nM), human A3 (Ki: 25.4 nM) and rat A1 (Ki: 1.47 nM). 1 Can be used to study renal failure, inflammatory lung disease and Alzheimer's disease.

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

hA2A/hCA XII modulator 1 is a potent antagonist of the hA2A adenosine receptor (hA2AAR), a triazolopyrazine that acts on hA2AAR (Ki: 6.4 nM), hA1AR (Ki: 4.819 μM), and hA3AR (Ki>30 μM). hA2A/hCA XII modulator 1 Also a potent inhibitor of human carbonic anhydrase XII (hCA XII), capable of acting on hCA XII (Ki: 6.2 nM), hCA II (Ki: 46 nM), hCA IX (Ki: 466 nM) and hCA I (Ki: 8.351 μM). hA2A/hCA XII modulator 1 exhibits potential for cancer research.