| 货号 | 2386/50 |
| 别名 | N-(3-Chlorophenyl)-N'-(4,5-dihydro-1 |
| 供应商 | Tocris |
| 生物活性 | Potent and selective non-competitive mGlu5 antagonist that displays inverse agonist properties; blocks mGlu5 constitutive activity in vitro(IC50 = 87 nM). Acts at an allosteric modulatory site shared with MPEP and binds the mGlu5 receptor with Kd values of 54 and 31 nM for rat and human receptors respectively. Displays anxiolytic activity following oral administration in vivo; also exhibits analgesic properties. |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >99 % |
| 计算分子量 | 266.69 |
| 分子式 | C11H11N4O2Cl |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| CAS号 | 57653-26-6 |
| 参考文献 | Montanaet al (2009) The metabotropic glutamate receptor subtype 5 antagonist fenobam is analgesic and has improved in vivo selectivity compared with the prototypical antagonist 2-methyl-6-(phenylethynyl)-pyridine. J.Pharmacol.Exp.Ther. 330 834. PMID: 19515968. Porteret al (2005) Description of a clinically validated anxiolytic with mGlu5 antagonist properties. Neuropharmacology 49 (Suppl. 1) 267. Porteret al (2005) Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J.Pharmacol.Exp.Ther. 315 711. PMID: 16040814. |