| 货号 | 4415/50 |
| 别名 | 7-Cyclobutyl-3-(2,6-difluorophenyl) |
| 供应商 | Tocris |
| 生物活性 | Subtype-selective GABAA partial agonist (Ki values are 0.21, 0.22, 0.23 and 0.40 for α3, α1, α5 and α2 respectively); occupies the benzodiazepine site of GABAA receptors. Displays greater agonist efficacy at α3 compared to α1. Exhibits anxiolytic and non-sedating properties in rodent models. Brain penetrant. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >99 % |
| 计算分子量 | 397.38 |
| 分子式 | C19H17F2N7 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 50 mM in ethanol |
| 参考文献 | Atacket al (2011) MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans. J.Psychopharmacol. 25 314. PMID: 20147571. Atacket al (2010) Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, primates, and humans. J.Pharmacol.Exp.Ther. 33217. de Haaset al (2008) Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABAAα2,3 subtype-selective agonist, compared to lorazepam and placebo in healthy male volunteers. J.Psychopharmacol. 22 24. PMID: 18187530. |