HTS025M - ChemiSCREEN™ MCH1 Melanin-Concentrating Hormone Receptor Membrane Preparation

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    Melanin-concentrating hormone (MCH) is a cyclic, 19 amino acid peptide produced in the lateral hypothalamus and other regions of the mammalian brain (Bittencourt et al., 1992). When administered intracerebrally or overexpressed transgenically in rodents, MCH stimulates food intake and weight gain (Ludwig et al., 2001). A receptor for MCH, previously identified as an orphan receptor SLC-1 and renamed MCH1, has been identified in humans and rodents. Consistent with a role in hypothalmic control of feeding behavior, MCH1 is expressed in in the ventromedial and dorsomedial nuclei of the hypothalamus (Chambers et al., 1999). Genetic ablation and pharmacological antagonism of MCH1 in rodents results in resistance to obesity caused by a high fat diet or leptin deficiency (Borowsky et al., 2002; Segal-Lieberman, et al., 2003; Shearman et al., 2003; Marsh et al., 2002; Chen et al., 2002). Thus, MCH1 is an attractive target for obesity. MCH1membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level GPCR surface expression; thus, they are ideal HTS tools for screening for agonists and antagonists of MCH1.

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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 MCHR1 cDNA encoding MCH1 (Accession number NM_005297).
    Host Cell: Chem-1, adherent mammalian cell line no detectable endogenous MCH1 expression.
    Reference 1: 1. Bittencourt J.C., et al. (1992) The melanin-concentrating hormone system of the rat brain: an immuno- and hybridization histochemical characterization. J. Comp. Neurol. 319: 218-45.
    Reference 2: 2. Borowsky B., et al. (2002) Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist. Nat. Med. 8: 825-30.
    Reference 3: 3. Chambers J., et al. (1999) Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1. Nature 400: 261-5.
    Reference 4: 4. Chen Y., et al. (2002) Targeted disruption of the melanin-concentrating hormone receptor-1 results in hyperphagia and resistance to diet-induced obesity. Endocrinology 143: 2469-77.
    Reference 5: 5. Ludwig D.S., et al. (2001) Melanin-concentrating hormone overexpression in transgenic mice leads to obesity and insulin resistance. J. Clin. Invest. 107: 379-86.
    Reference 6: 6. Marsh D.J., et al. (2002) Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism. Proc. Natl. Acad. Sci. USA 99: 3240-5.