HTS023M - ChemiSCREEN™ CRF1 Receptor Membrane Preparation

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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). CRF1 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 CRF1 interactions with its ligands. The membrane preparations exhibit a Kd of 1 nM for [125I]-sauvagine.

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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: Human CRF1 (Accession number X72304)
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous CRF1 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. 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. Kehne J and De Lombaert S (2002) Non-peptidic CRF1 receptor antagonists for the treatment of anxiety, depression and stress disorders. Curr. Drug Targets CNS Neurol. Disord. 1: 467-493.