CAS NO: | 873551-53-2 |
包装: | 10mg |
市场价: | 4140元 |
Cas No. | 873551-53-2 |
Canonical SMILES | O=C(N(C(C)C)C)N1CC=C(C2=C(C)N(C3=C(F)N=CC=C3)N=N2)CC1 |
分子式 | C18H23FN6O |
分子量 | 358.41 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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. 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 |