Calcium Flux Assay

HTS025C - ChemiSCREEN™ Human Recombinant MCHR1 Melanin-concentrating Hormone Receptor Calcium-Optimized Stable Cell Line

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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 MCHR1, has been identified in humans and rodents.  Consistent with a role in hypothalmic control of feeding behavior, MCHR1 is expressed in in the ventromedial and dorsomedial nuclei of the hypothalamus (Chambers et al., 1999).  Genetic ablation and pharmacological antagonism of MCHR1 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, MCHR1 is an attractive target for obesity.  The cloned MCHR1-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant MCHR1 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 MCHR1 and its ligands.  

    Additional Resource :  HTS025C052215 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: Calcium Flux Assay
    Host Cell: Chem-1, an adherent cell line expressing the promiscuous G-protein, Gα15.
    Exongenous Gene Expression: Human MCHR1 cDNA (Accession Number: NM_005297) and promiscuous G protein are expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    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.