Catalog Number: 2921
Chemical Name: 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine hydrochloride
Biological Activity
Potent, selective and non-competitive mGlu5 antagonist (IC50 = 5 nM in Ca2+-flux assay; Ki= 16 nM). Displays anxiolytic activity in vivo and is orally active.
Technical Data
  • M.Wt:
    236.72
  • Formula:
    C11H8N2S.HCl
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    1186195-60-7
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.
Additional Information
Licensing Caveats:
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
Background References
  1. Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice.
    Bradbury et al.
    J.Pharmacol.Exp.Ther., 2005;313:395
  2. 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
    Roppe et al.
    Bioorg.Med.Chem.Lett., 2004;14:3993
  3. Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABAA signaling.
    Klodzinska et al.
    Neuropharmacology, 2004;47:342
  4. 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.
    Cosford et al.
    J.Med.Chem., 2003;46:204
  5. Reduced stress-induced hyperthermia in mGluR5 knockout mice.
    Brodkin et al.
    Eur.J.Neurosci., 2002;16:2241

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