HTS146RTA - Ready-to-Assay™ mGlu2 Metabotropic Glutamate Receptor Frozen Cells

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    Glutamate is a main excitatory neurotransmitter in the central nervous system, and it plays a role in learning, memory and neurotoxicity. The biological actions of glutamate are mediated by ionotropic and metabotropic glutamate receptors, which are ion channels and GPCRs respectively. Metabotropic glutamate receptors (mGluRs) are members of the class 3 G-protein coupled receptor family, which are characterized by a large extracellular domain. They are further classified into group I, II, and III mGluRs on the basis of their sequence identity, pharmacology, and signal transduction mechanism. Group I (mGlu1 and mGlu5) couple to the phospholipase C pathway through Gαq, whereas group II (mGlu2 and mGlu3) and group III (mGlu4, mGlu6, mGlu7, and mGlu8) negatively couple to the adenylyl cyclase pathway though Gαi (Conn and Pin, 1997). Agonists of the Group II metabotropic glutamate receptors, mGlu2 and mGlu3, display efficacy in animal models of anxiety and psychosis. A key role for mGlu2 in mediating these effects is indicated by the observation that selective allosteric potentiator of mGlu2 also retains antipsychotic-like activities in mice (Galici et al., 2005). In addition, mGlu2/3 agonists display analgesic activity in animal models (Jones et al., 2005). Cloned human mGlu2-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant mGlu2 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 agonists and antagonists at mGlu2.

    Additional Resource :  HTS146RTA100214 Datasheet

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    Item Unit of Measure: PK
    Quantity: Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial. Fifty (50) mL of Media Component.
    Storage: Vials are to be stored in liquid N2. Media Component at 4ºC (-20ºC for prolonged storage).
    Applications: Calcium Flux Assay
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein.
    Exongenous Gene Expression: GRM2 cDNA (Accession Number: NM_000839- see CODING SEQUENCE below) expressed from a proprietary pHS plasmid.
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Conn PJ and Pin JP (1997) Pharmacology and functions of metabotropic glutamate receptors. Annu. Rev. Pharmacol. Toxicol. 37: 205-37.
    Reference 2: 2. Galici R et al. (2005) A selective allosteric potentiator of metabotropic glutamate (mGlu) 2 receptors has effects similar to an orthosteric mGlu2/3 receptor agonist in mouse models predictive of antipsychotic activity. J. Pharmacol. Exp. Ther. 3
    Reference 3: 3. Galici R et al. (2006) Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice. J. Pharmacol. Exp. Ther. 318: 173-185.
    Reference 4: 4. Jones CK et al. (2005) Analgesic effects of the selective group II (mGlu2/3) metabotropic glutamate receptor agonists LY379268 and LY389795 in persistent and inflammatory pain models after acute and repeated dosing. Neuropharmacology 49 Suppl 1:2
    Reference 5: 5. Kowal D et al. (2003) Functional calcium coupling with the human metabotropic glutamate receptor subtypes 2 and 4 by stable co-expression with a calcium pathway facilitating G-protein chimera in Chinese hamster ovary cells. Biochem. Pharmacol. 6
    Reference 6: 6. Schoepp DD et al. (1997) The novel metabotropic glutamate receptor agonist 2R,4R-APDC potentiates stimulation of phosphoinositide hydrolysis in the rat hippocampus by 3,5-dihydroxyphenylglycine: evidence for a synergistic interaction between group