Name | FTIDC |
---|---|
Supplier | Tocris Bioscience |
Catalog | 2407 |
Prices | $309.00 |
Sizes | 10 mg |
Function Type | Modulator |
Cas Number | 873551-53-2 |
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 |
Formula | C18H23FN6O |
Molecular Weight | 358.41 |
Purity | >98 % |
Description | Potent and selective mGlu 1 receptor negative allosteric modulator (IC 50 values are 5.8 and 6200 nM for mGlu 1 and mGlu 5 respectively). Also acts as an mGlu 1 receptor inverse agonist (IC 50 = 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 mGlu 1 -expressing CHO cells. Inhibits nociceptive behavior, and exhibits anxiolytic and antipsychotic effects in vivo . Orally active. |
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Suzuki G, Kimura T, Satow A, Kaneko N, Fukuda J, Hikichi H, Sakai N, Maehara S, Kawagoe-Takaki H, Hata M, Azuma T, Ito S, Kawamoto H, Ohta H. J Pharmacol Exp Ther. 2007 Jun;321(3):1144-53. Epub 2007 Mar 14.
Ito S, Satoh A, Nagatomi Y, Hirata Y, Suzuki G, Kimura T, Satow A, Maehara S, Hikichi H, Hata M, Kawamoto H, Ohta H. Bioorg Med Chem. 2008 Nov 15;16(22):9817-29.
Satow A, Maehara S, Ise S, Hikichi H, Fukushima M, Suzuki G, Kimura T, Tanak T, Ito S, Kawamoto H, Ohta H. J Pharmacol Exp Ther. 2008 Aug;326(2):577-86.