HTS047M - ChemiScreen™ A1 Adenosine Receptor Membrane Preparation

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    Extracellular adenosine mediates a multitude of biological effects, including wakefulness, antiarrythmia, bronchoconstriction and response to ischemia and oxidative stress. A family of four GPCR adenosine receptors, A1, A2A, A2B and A3, is responsible for these effects. The A1 receptor, which couples to Gi/o, is most highly expressed in brain, and mediates endogenous antinociception and neuronal response to hypoxia (Fredholm et al., 2001). A1 is also expressed in kidney, where it contributes to tubuloglomerular feedback. A1 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of agonists and antagonists at A1. The membrane preparations exhibit a Kd of 1.2 nM for [3H]-Cyclopentyl-1, 3-dipropylxanthine, 8-[dipropyl-2, 3-3H (N)]. With 10 mg/well A1 Membrane Prep and 20 nM [3H]-DPCPX, a greater than 7-fold signal-to-background ratio is obtained.

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles.
    Applications: Radioligand Binding Assay
    Species: Human A1 (Accession number S45235)
    Host Cell: Chem-3, a suspension mammalian cell line without any endogenous A1 expression.
    Reference 1: 1. Fredholm, BB et al. (2001) International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors. Pharmacol. Rev. 53: 527-552.