Application

Human NTR1 / NTS1 GPCR frozen cells for Calcium Flux FLIPR Assays.

Biochem/physiol Actions

GPCR Class: A Protein Target: NTR1/ NTS1 Target Sub-Family: Neurotensin

Cell Line Description

GPCR Cell Lines Host cells: Chem-1

Components

Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial. Fifty (50) mL of Media Component.

Disclaimer

This product contains genetically modified organisms (GMO). Within the EU GMOs are regulated by Directives 2001/18/EC and 2009/41/EC of the European Parliament and of the Council and their national implementation in the member States respectively.

General description

Millipore’;s Ready-to-Assay GPCR frozen cells are designed for simple, rapid calcium assays with no requirement for intensive cell culturing. Millipore has optimized the freezing conditions to provide cells with high viability and functionality post-thaw. The user simply thaws the cells and resuspends them in media, dispenses cell suspension into assay plates and, following over night recovery, assays for calcium response.

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).
Millipore’;s 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.