General paperMolecular cloning, functional expression and pharmacological characterization of the human metabotropic glutamate receptor type 4
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Tetracycline-based system for controlled inducible expression of group III metabotropic glutamate receptors
2015, Journal of Biomolecular ScreeningAFQ056/mavoglurant, a novel clinically effective mGluR5 antagonist: Identification, SAR and pharmacological characterization
2014, Bioorganic and Medicinal ChemistryCitation Excerpt :1H NMR (500 MHz, DMSO-d6, rotamers 2:1): δ 7.85 (d, 1H), 7.30–7.15 (m, 4H), 7.06 (d, 1H), 6.62 (m, 1H), 5.8 (b, 1H), 4.49 (m, 0.33H), 4.30 (m, 0.67H), 3.95 (t, 0.67H), 3.25 (q, 0.67H), 3.58 (m, 0.66H), 2.70, 2.58 (2 m, 1H), 2.30, 2.29 (2s, 3H), 2.10–1.10 (m, 8H). The generation and the culturing of the cell lines stably expressing hmGluR1b, hmGluR2, hmGluR4, hmGluR5a and hmGluR7 were described in detail previously.18,32–34 Cell culture was performed essentially as described by Flor et al.32 Briefly, cells were cultured in glutamate free medium composed of DMEM lacking l-glutamate (without phenol red, Gibco, #11880-028) containing a reduced concentration of 2 mM l-glutamine (Gibco, #25030-024), supplemented with 0.046 mg/ml proline (Sigma, #P0380), 10% dialyzed fetal calf serum (Gibco, #26300-061) and 50 mg/ml geneticin (G-418 sulphate, Gibco, #11811-031).
Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior
2014, Journal of Biological ChemistryCitation Excerpt :All other chemicals were of reagent grade and obtained from Fluka (Buchs, Switzerland), Merck, Serva (Heidelberg, Germany), or Sigma-Aldrich. Generation, culture, and pharmacological characterization of stable CHO or L cell lines transfected with mammalian mGlu2, mGlu4, mGlu5a, mGlu6, mGlu6/7, mGlu7a, mGlu7b, mGlu7/5a, mGlu7/6, GABAB, arginine vasopressin 1A (V1a), and oxytocin receptors were conducted as described recently (8, 22, 36–39). cDNAs encoding human mGlu6 and mGlu7b were described previously (8, 40).
Metabotropic glutamate receptors: From the workbench to the bedside
2011, NeuropharmacologyCitation Excerpt :Accession numbers: NP_000832 (human); NP_073157 (rat); NP_001013403 (mouse). Chromosomal location: 6p21.3 (human); 20p12 (rat); 17A3.3 (mouse) (Tanabe et al., 1992; Kuramoto et al., 1994; Flor et al., 1995b; Barbon et al., 2000a). Gene name: GRM7 (human); Grm7 (rat, mouse).
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
2003, Biochemical PharmacologyCitation Excerpt :Advantages of the FLIPR assay are compatibility with high-throughput applications, elimination of the use of radioactivity and the ability to detect activity of agonists, antagonists, and allosteric modulators (although not addressed here) in the same assay. Importantly, both agonist and antagonist potencies were in very good agreement with those determined previously using other assay formats [7,8,12–14,19,20]. In cases where modest differences in agonist activities were observed, these are likely attributed to several factors such as the use of different cell lines between investigators, coupling efficiency of native vs. chimeric G-proteins, and measurement of different functional endpoints.