HTS034C - ChemiScreen™ NTR1 Neurotensin Receptor Stable Cell Line

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    Neurotensin is a 13 amino acid peptide that induces hypothermia and mediates analgesia when administered centrally, and also mediates the behavioral effects of antipsychotic drugs in rodents (Kinkead and Nemeroff, 2004).  In addition, several intestinal functions, such as contractility and inflammation, are mediated by neurotensin (Castagliuolo et al., 1999).  The actions of neurotensin are mediated by two GPCRs, NTR1 (or NTS1) and NTR2 (or NTS2).  NTR1 knockout mice are resistant to the hypothermic, analgesic and contractile effects of neurotensin, indicating that NTR1 is the primary mediator of these effects (Pettibone et al., 2002).  Small molecule antagonists, including SR48692 and SR142948A, that are partially selective for NTR1 also interfere with the biological effects of neurotensin (Labbé-Jullié et al., 1998). Cloned human NTR1-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant NTR1 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 NTR1 and neurotensin.

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    Item Unit of Measure: PK
    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 rat hematopoietic cell line expressing endogenous Gα15 protein
    Exogenous Gene Expression: Full-length human NTR1 cDNA (Accession Number: NM_002531); see CODING SEQUENCE below) expressed from a proprietary pHS plasmid.
    GMO: This product contains genetically modified organisms.
    Reference 1: "1. Castagliuolo I., et al. (1999) Neurotensin is a proinflammatory neuropeptide in colonic inflammation. J. Clin. Invest. 103: 843-849.
    Reference 2: 2. Kinkead B. and Nemeroff C. (2004) Neurotensin, schizophrenia, and antipsychotic drug action. Int. Rev. Neurobiol. 59: 327-349.
    Reference 3: 3. Labbé-Jullié C., et al. (1998) Mutagenesis and modeling of the neurotensin receptor NTR1: Identification of residues that are critical for binding SR48692, a nonpeptide neurotensin antagonist. J. Biol. Chem. 273: 16351-16357.
    Reference 4: 4. Pettibone D.J., et al. (2002) The effects of deleting the mouse neurotensin receptor NTR1 on central and peripheral responses to neurotensin. J. Pharmacol. Exp. Ther. 300: 305-313.