1. Signaling Pathways
  2. GPCR/G Protein
  3. Adenosine Receptor

Adenosine Receptor

P1 receptor

Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes have been cloned and identified in different tissues. These receptors have distinct localization, signal transduction pathways and different means of regulation upon exposure to agonists. A key property of some of Adenosine receptors is their ability to serve as sensors of cellular oxidative stress, which is transmitted by transcription factors, such as NF-κB, to regulate the expression of ARs. The importance of Adenosine receptors in the regulation of normal and pathological processes such as sleep, the development of cancers and in protection against hearing loss will be examined.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-103163
    (±)-5'-Chloro-5'-deoxy-ENBA
    Agonist
    (±)-5'-Chloro-5'-deoxy-ENBA is an agonist of A1AR. (±)-5'-Chloro-5'-deoxy-ENBA produces hypothermia in mice.
    (±)-5'-Chloro-5'-deoxy-ENBA
  • HY-W088152R
    8-Bromotheophylline (Standard)
    8-Bromotheophylline (Standard) is the analytical standard of 8-Bromotheophylline. This product is intended for research and analytical applications. 8-Bromotheophylline can be used for the synthesis of the Oxazolo[2,3-f]purinediones, which are evaluated for their affinity at adenosine A1 and A2A receptors.
    8-Bromotheophylline (Standard)
  • HY-B0809S1
    Theophylline-d3
    Inhibitor
    Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline-d<sub>3</sub>
  • HY-100937S
    DPCPX-d4
    Antagonist
    DPCPX-d4 (PD 116948-d4) is deuterium-labeled DPCPX (HY-100937).
    DPCPX-d<sub>4</sub>
  • HY-101139B
    Xanthine amine congener trihydrochloride
    Antagonist
    Xanthine amine congener trihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2?receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model.
    Xanthine amine congener trihydrochloride
  • HY-136702
    L-97-1
    Antagonist
    L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation.
    L-97-1
  • HY-103182R
    PSB-1115 (Standard)
    Antagonist
    PSB-1115 (Standard) is the analytical standard of PSB-1115. This product is intended for research and analytical applications. PSB-1115 is a selective A2B Adenosine Receptor antagonist. PSB-1115 inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh).
    PSB-1115 (Standard)
  • HY-B1505R
    Acefylline (Standard)
    Antagonist
    Acefylline (Standard) is the analytical standard of Acefylline. This product is intended for research and analytical applications. Acefylline, a xanthine derivative, is an adenosine receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline can be used in asthma research.
    Acefylline (Standard)
  • HY-105138
    Adentri
    Antagonist
    Adentri (CVT-124) is a potent and A1-adenosine selective antagonist with a Ki of 0.45 nM at cloned human A1-receptors. Adentri can be utilized in cardiovascular research.
    Adentri
  • HY-116837
    LUF5831
    Agonist
    LUF5831 is a non-adenosine agonist with an affinity of Ki=18 nM for adenosine A1 receptor.
    LUF5831
  • HY-B1742R
    Proxyphylline (Standard)
    Antagonist
    Proxyphylline (Standard) is the analytical standard of Proxyphylline. This product is intended for research and analytical applications. Proxyphylline is a methylxanthine derivative used as a cardiac stimulant, vasodilator and bronchodilator.
    Proxyphylline (Standard)
  • HY-N0092S4
    Inosine-13C3
    Agonist
    Inosine-13C3 is a 13C-labeled Inosine that can be used in pharmacokinetic studies of Inosine. Inosine is an agonist of adenosine receptors A1R and A2AR with anti-inflammatory immunomodulatory, antinociceptive and neuroprotective effects.
    Inosine-<sup>13</sup>C<sub>3</sub>
  • HY-103186R
    MRS-1706 (Standard)
    Antagonist
    MRS-1706 (Standard) is the analytical standard of MRS-1706. This product is intended for research and analytical applications. MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction.
    MRS-1706 (Standard)
  • HY-110170
    Dansyl-NECA
    Antagonist
    Dansyl-NECA (compound 1) is a dansyl-labeled adenosine receptor antagonist.
    Dansyl-NECA
  • HY-14409
    Lu AA41063
    Antagonist
    Lu AA41063 is an adenosine A2A receptor antagonist that may be useful in the treatment of Parkinson's disease. Lu AA41063 has a Ki value of 5.9 nM and targets the human A2A receptor.
    Lu AA41063
  • HY-100937R
    DPCPX (Standard)
    Antagonist
    DPCPX (Standard) is the analytical standard of DPCPX. This product is intended for research and analytical applications. DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes.
    DPCPX (Standard)
  • HY-12365R
    Namodenoson (Standard)
    Agonist
    Namodenoson (Standard) is the analytical standard of Namodenoson. This product is intended for research and analytical applications. Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
    Namodenoson (Standard)
  • HY-155467
    MRS7935
    Modulator
    MRS7935 (compound 15) is an A1AR positive allosteric modulator (PAM) with an EC50 of approximately 2 μM.
    MRS7935
  • HY-151387
    A2AAR antagonist 1
    Antagonist
    A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a Ki value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases.
    A2AAR antagonist 1
  • HY-115862
    Benzo[c][1,8]naphthyridin-6(5H)-one
    Benzo[c][1,8]naphthyridin-6(5H)-one exhibits low micromolar affinity to human adenosine receptor (AR) A1 and hA2A, with Ki of 4.6 and 4.8 μM. Benzo[c][1,8]naphthyridin-6(5H)-one is inhibitor for poly ADP-ribose polymerase-1 (PARP-1) and aurora kinase A, with IC50 of 0.311 and 5.5 μM.
    Benzo[c][1,8]naphthyridin-6(5H)-one
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