Catalog Number: 5000
Chemical Name: 4-[1-(2-Fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-3,6-dihydro-N-methyl-N-(1-methylethyl)-1(2H)-pyridinecarboxamide
Biological Activity
Potent and selective mGlu1 receptor negative allosteric modulator (IC50 values are 5.8 and 6200 nM for mGlu1 and mGlu5 respectively). Also acts as an mGlu1 receptor inverse agonist (IC50 = 7 nM) in the absence of ligand. Exhibits no effect at group II/III mGlu receptors. Inhibits L-glutamate-induced increases in intracellular calcium in mGlu1-expressing CHO cells. Inhibits nociceptive behavior, and exhibits anxiolytic and antipsychotic effects in vivo. Orally active.
Technical Data
  • M.Wt:
    358.41
  • Formula:
    C18H23FN6O
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    873551-53-2
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Pharmacological effects of the metabotropic glutamate receptor 1 antagonist compared with those of the metabotropic glutamate receptor 5 antagonist and metabotropic glutamate receptor 2/3 agonist in rodents: detailed investigations with a selective allost
    Satow et al.
    J.Pharmacol.Exp.Ther., 2008;326:577
  2. Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(
    Suzuki et al.
    J.Pharmacol.Exp.Ther., 2007;321:1144
  3. Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.
    Ito et al.
    Bioorg.Med.Chem., 2008;16:9817

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