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.
Licensing Information
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)
Technical Data
| M. Wt | 236.72 |
| Formula | C11H8N2S.HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1186195-60-7 |
| PubChem ID | 45073467 |
| InChI Key | YCIOJDKGCWAHLR-UHFFFAOYSA-N |
| Smiles | CC1=NC(C#CC2=CN=CC=C2)=CS1.Cl |
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.
Solubility Data
| DMSO | 23.67 | 100 |
| water | 23.67 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 236.72. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 1 mM | 4.22 mL | 21.12 mL | 42.24 mL |
| 5 mM | 0.84 mL | 4.22 mL | 8.45 mL |
| 10 mM | 0.42 mL | 2.11 mL | 4.22 mL |
| 50 mM | 0.08 mL | 0.42 mL | 0.84 mL |
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Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDSReferences
References are publications that support the products\' biological activity.
Bradbury et al (2005) Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice. J.Pharmacol.Exp.Ther. 313 395 PMID: 15590770
Roppe et al (2004) 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. Bioorg.Med.Chem.Lett. 14 3993 PMID: 15225713
Klodzinska et al (2004) Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABAA signaling. Neuropharmacology 47 342 PMID: 15275823
Cosford et al (2003) 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. J.Med.Chem. 46 204 PMID: 12519057
Brodkin et al (2002) Reduced stress-induced hyperthermia in mGluR5 knockout mice. Eur.J.Neurosci. 16 2241 PMID: 12473093
Keywords: MTEP hydrochloride, supplier, Potent, selective, mGlu5, mGluR5, antagonists, mGlur, Group, I, Receptors, Glutamate, Metabotropic, merck, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
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