HTS048L - ChemiBrite™ Human A2A Adenosine Receptor Calcium-Optimized Stable Cell Line

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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 G protein-coupled adenosine receptors, A1, A2A, A2B and A3, is responsible for these effects. A2A, which couples to Gs, is expressed in basal ganglia and immune cells. A2A reduces ischemia-induced inflammation; however, A2A antagonists protect from neurodegeneration during Parkinson's disease (Chen, 2003). Caffeine, the most widely used psychoactive drug, is a nonselective adenosine receptor antagonist, but its psychomotor stimulant affect is attributed to A2A expressed on striatal projection neurons (Fisone et al., 2004). Cloned A2A receptor-expressing ChemiBrite cells were made by stable transfection of HEK293 cells with ChemiBrite clytin and the receptor and a promiscuous G protein to couple the receptor to the calcium signaling pathway. These stability-tested cells are ready for luminescent analysis of agonists, antagonists and modulators at the A2A receptor.

    Additional Resource :  HTS048L080714 Datasheet

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    Contents: 2 vials of mycoplasma-free cells, 1 ml per vial.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay, cAMP Accumulation
    Host Cell: HEK293
    Exongenous Gene Expression: Human ADORA2A cDNA (Accession Number: BC017830- see CODING SEQUENCE below) and a proprietary mutant clytin photoprotein and promiscuous G protein expressed in a bicistronic vector.
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Chen JF (2003) The adenosine A2A receptor as an attractive target for Parkinson's disease treatment. Drug News Perspect. 16: 597-604
    Reference 2: 2. Fisone G et al. (2004) Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol. Life Sci. 61: 857-72.
    Reference 3: 3. Fredholm, BB et al. (2001) International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors. Pharmacol. Rev. 53: 527-552
    Reference 4: 4. Cooper et al. (1995) Adenosine Receptor-Induced cyclic AMP generation and inhibition of 5-hydroxytryptamine release in human platelets. Br J Clin Pharm 40:43-50