Adenosine Receptors

Adenosine receptor agonists and antagonists target A1, A2A, A2B and A3, the four G protein-coupled adenosine receptors. The International Union of Pharmacology (IUPHAR) set out this nomenclature in 2001. A1 and A3 receptors usually inhibit adenylyl cyclase, while A2A and A2B receptors stimulate it. In 2008 the human A2A receptor was crystallized bound to an antagonist at 2.6 Å resolution. Ligands in this category include the A2A agonist CGS 21680 HCl Hydrate, the A2A antagonist istradefylline and the A3 agonist IB-MECA. Xanthines such as theophylline block several subtypes, and 5-Iodotubercidin inhibits adenosine kinase, which phosphorylates adenosine.

3 Items

  • Adenosine-2'-monophosphate
    Cat. No.
    A57879

    Adenosine-2'-monophosphate

    Synonyms: 2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate

    Adenosine-2'-monophosphate (2'-AMP) functions primarily as an adenosine receptor activator. This compound is metabolized to extracellular adenosine through the extracellular 2’,3’-cAMP-adenosine pathway, playing a crucial role in modulating immune responses. Research indicates that 2'-AMP inhibits lipopolysaccharide (LPS)-induced production of TNF-α and CXCL10 via activation of the A2A receptor, making it a valuable tool in studies of inflammation and immune regulation.

    2 mg
    $45.00
    5 mg
    $65.00
    All 3 sizes
  • Adenosine A1 receptor activator T62
    Cat. No.
    A57914

    Adenosine A1 receptor activator T62

    Adenosine A1 receptor activator T62 is an allosteric enhancer of the adenosine A1 receptor. It exhibits significant antinociceptive properties in animal models of acute pain and effectively alleviates hypersensitivity in models of inflammatory and nerve-injury pain. This compound is valuable for research focused on pain management and the modulation of pain pathways.

    1 mg
    $50.00
    5 mg
    $110.00
    All 7 sizes
  • A3AR agonist 5
    Cat. No.
    A57996

    A3AR agonist 5

    A3AR Agonist 5 is a potent activator of the A3 adenosine receptor (A3AR), exhibiting EC50 and Ki values of 0.14 nM and 6.36 nM for cAMP and human A3 receptors, respectively. This compound is valuable for research into pain modulation and inflammation, making it a significant tool for studies examining adenosine receptor signaling pathways and their therapeutic implications.

    Out of stock

    All 3 sizes

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