HTS024C - ChemiSCREEN™ Human CRF2 Receptor Calcium-Optimized Stable Cell Line

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HTS024C
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    The corticotropin-releasing factor receptors, CRF1 and CRF2, are Gs-coupled GPCRs expressed in the brain, blood vessels and intestine that bind to several neuropeptides, including corticotropin-releasing factor (CRF) and urocortin, and the amphibian peptide sauvagine (Lovenberg et al., 1995;  Bale and Vale, 2004).  In addition, two peptides, urocortin II (Ucn II) and urocortin III (Ucn III), bind selectively and with high affinity to CRF2 (Lewis et al., 2001).  The CRF peptides and their receptors play important roles in stress mediated by the hypothalamic-pituitary-adrenal axis in animal models, and possibly in depression and anxiety in humans, although the contributions of CRF1 and CRF2 appear to be distinct (Bale and Vale, 2004;  Risbrough et al., 2004)  In addition, CRF1 and CRF2 differentially alter feeding behavior, gastric motility and vascular tone (Zorrilla et al., 2004;  Martinez et al., 2004;  Wiley and Davenport, 2004).  The cloned human CRF2-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant CRF2 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 CRF2 and its ligands.

    Additional Resource :  HTS024C050615 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 CRF2 cDNA (Accession Number: NM_001883) 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. Lewis K et al. (2001) Identification of urocortin III, an additional membrer of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. USA 98: 7570-7575.
    Reference 3: 3. Lovenberg TW et al. (1995) Cloning and characterization of a functionally distinct corticoptropin-releasing factor receptor subtype from rat brain. Proc. Natl. Acad. Sci. USA 92: 836-840.
    Reference 4: 4. Martinez V et al. (2004) Central CRF, urocortins and stress increase colonic transit via CRF1 receptors while activation of CRF2 receptors delays gastric transit in mice. J. Physiol. 556: 221-234 .
    Reference 5: 5. Risbrough VB et al. (2004) Corticotropin-releasing factor receptors CRF1 and CRF2 exert both additive and opposing influences on defensive startle behavior. J. Neurosci. 24: 6545-6552.
    Reference 6: 6. Wiley KE and Davenport AP (2004) CRF2 receptors are highly expressed in the human cardiovascular system and their cognate ligands urocortins 2 and 3 are potent vasodilators. Br. J. Pharmacol. 143: 508-514 .
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