| 货号 | 2921/50 |
| 别名 | 3-((2-Methyl-1,3-thiazol-4-yl)ethyn |
| 供应商 | Tocris |
| 生物活性 | 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. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >99 % |
| 计算分子量 | 236.72 |
| 分子式 | C11H8N2S.HCl |
| 可溶性/溶解性 | Soluble to 100 mM in water and to 100 mM in DMSO |
| 参考文献 | Bradburyet 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. Klodzinskaet al (2004) Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABAA signaling. Neuropharmacology 47 342. PMID: 15275823. Roppeet 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. Cosfordet 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. Brodkinet al (2002) Reduced stress-induced hyperthermia in mGluR5 knockout mice. Eur.J.Neurosci. 16 2241. PMID: 12473093. |