Calcium Flux Assay

HTS023C - ChemiSCREEN™ Human CRF1 Receptor Calcium-Optimized Stable Cell Line

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HTS023C
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    The CRF1 receptor is a Gs-coupled GPCR expressed in the brain and pituitary gland that binds to several neuropeptides, including corticotropin-releasing factor (CRF) and urocortin, and the amphibian peptide sauvagine (Chen et al., 1993;  Dautzenberg and Hauger, 2002;  Bale and Vale, 2004).  CRF plays a predominant role in stress response mediated by the hypothalamic-pituitary-adrenal axis, and alterations in CRF and its receptors CRF1 and CRF2 appear to be linked to depression and anxiety (Holsboer, 1999;  Bale and Vale, 2004).  A number of small molecule antagonists of the CRF1 receptor have been characterized, including R121919, SC241, NBI27914, antalarmin, DMP-696, and CP 154,526.  When delivered in animal models of psychiatric disorders, these antagonists display effectiveness in reducing stress-related behaviors (Kehne and De Lombaert, 2002).  The cloned human CRF1-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant CRF1 expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway.  Thus, the cell line is an ideal tool for screening for antagonists of interactions between CRF1 and its ligands.

    Additional Resource :  HTS023C050615 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: cAMP Accumulation
    Host Cell: Chem-1, an adherent cell line expressing the promiscuous G-protein, Gα15.
    Exongenous Gene Expression: Human CRF1 cDNA (Accession Number: X72304) and promiscuous G protein are expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Bale TL and Vale WW (2004) CRF and CRF receptors: role in stress responsivity and other behaviors. Annu. Rev. Pharmacol. Toxicol. 44: 525-557.
    Reference 2: 2. Chen R., et al. (1993) Expression cloning of a human corticotropin-releasing factor receptor. Proc. Natl. Acad. Sci. USA 90: 8967-8971.
    Reference 3: 3. Dautzenberg FM and Hauger RL (2002) The CRF peptide family and their receptors: yet more partners discovered. Trends Pharmacol. Sci. 23: 71-77.
    Reference 4: 4. Holsboer F (1999) The rationale for cotricotropin-releasing hormone receptor (CRH-R) antagonists to treate depression and anxiety. J. Psychiatr. Res. 33: 181-214.
    Reference 5: 5. Holsboer F (1999) The rationale for cotricotropin-releasing hormone receptor (CRH-R) antagonists to treate depression and anxiety. J. Psychiatr. Res. 33: 181-214.
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