HTS024M - ChemiSCREEN™ CRF2 Neuropeptide Receptor Membrane Preparation

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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). CRF2 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 antagonists of CRF2 interactions with its ligands. The membrane preparations exhibit a Kd of 0.65 nM for [125I]-sauvagine. With 5 mg/well CRF2 Membrane Prep and 0.35 nM [125I]-sauvagine, a greater than 20-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. For maximum recovery of product, centrifuge original vial
    Applications: Radioligand Binding Assay
    Species: Full-length human CRHR2 cDNA encoding CRF2 (Accession number NM_001883)
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous CRF2 expression.
    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 member 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.