HTS034M - ChemiSCREEN™ NTR1 Neurotensin Receptor Membrane Preparation

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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). NTR1 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 neurotensin/NTR1 interactions. The membrane preparations exhibit a Kd of 1.5 nM for [125I]-neurotensin.

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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.
    Applications: Radioligand Binding Assay
    Host Cell: Chem-2, a suspension mammalian cell line without any endogenous NTR1 expression.
    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.