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 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 873551-53-2 |
| PubChem ID | 11245287 |
| InChI Key | CJTLKLBSIFQKNT-UHFFFAOYSA-N |
| Smiles | O=C(N(C(C)C)C)N1CC=C(C2=C(C)N(C3=C(F)N=CC=C3)N=N2)CC1 |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.84 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 358.41. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.79 mL | 13.95 mL | 27.9 mL |
| 5 mM | 0.56 mL | 2.79 mL | 5.58 mL |
| 10 mM | 0.28 mL | 1.4 mL | 2.79 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Suzuki et al (2007) 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( J.Pharmacol.Exp.Ther. 321 1144 PMID: 17360958
Ito et al (2008) Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist. Bioorg.Med.Chem. 16 9817 PMID: 18849168
Satow et al (2008) 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 J.Pharmacol.Exp.Ther. 326 577 PMID: 18487514
Keywords: FTIDC, supplier, potent, selective, negative, allosteric, modulators, NAM, metabotropic, glutamate, receptors, mglu1, anxiolytic, antipsychotic, antinociceptive, orally, acive, in, vivo, mGluR1, inverse, agonists, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
