| 货号 | 5000/10 |
| 别名 | 4-[1-(2-Fluoro-3-pyridinyl)-5-methy |
| 供应商 | Tocris |
| 生物活性 | 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. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 358.41 |
| 分子式 | C18H23FN6O |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| 参考文献 | Itoet 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. Satowet 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 allosteric metabotropic glutamate receptor 1 antagonist, FTIDC [4-[1-(2-fluoropyridine-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide]. J.Pharmacol.Exp.Ther. 326 577. PMID: 18487514. Suzukiet 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(2H)-carboxamide (FTIDC). J.Pharmacol.Exp.Ther. 321 1144. PMID: 17360958. |