| CAS |
No.195055-03-9 |
| 英文名称 |
R121919 |
| 分子式 |
C22H32N6 |
| 分子量 |
380.53 |
| 溶解性 |
Soluble in DMSO/Ethanol |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 靶点 |
CRFR |
| 通路 |
GPCR & G Protein |
| 背景说明 |
R121919是一种高效的促肾上腺皮质激素释放因子受体 1 （CRF1）小分子受体拮抗剂，具有抗抑郁和抗焦虑活性，抑制 CRF1 受体、 CRF2 受体和 CRF 结合蛋白。 |
| 生物活性 |
R121919 (NBI30775) is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 has antidepressant and anxiolytic effects. R121919 alleviates defensive withdrawal in rats.[1-3] |
| In Vitro |
R121919 是一种强效小分子 CRF1 受体拮抗剂，对 CRF1 受体具有高亲和力，但对 CRF2 受体、CRF 结合蛋白或 70 种其他受体类型的活性较弱 1000 倍以上[1]。 |
| In Vivo |
R121919 (NBI30775) 剂量依赖性地降低大鼠肾上腺皮质激素和皮质酮 (HY-B1618) 对束缚应激的反应。R121919 剂量为 10 mg/kg 时，血浆肾上腺皮质激素和皮质酮的峰值浓度分别为 9% 和 25%[1]。 R121919 可降低大剂量小鼠的焦虑水平-响应曲线[2]。 |
| 动物实验 |
Rats: For the restraint stress，R121919 is dissolved in an aqueous 70% (v/v) polyethylene glycol 400 solution， and serially diluted in this vehicle to the appropriate concentrations. The drug is injected i.v. in a volume of 1 mL/kg to Male Sprague-Dawley rats. For the defensive withdrawal experiments， R121919 solutions are made fresh the night before each experiment. R121919 is dissolved in a vehicle consisting of 5% (v/v) polyethoxylated castor oil[1]. Mice: R121919 is dissolved in an aqueous. The drug is administered orally (1 mL/100 g bodyweight) via a feeding tube to six to ten mice per group; the doses applied are 0.5， 1.0 and 5.0 mg/kg for the DBA/2NCRL mice and 1.0， 5.0， and 30 mg/kg for the DBA/2Ola strain; an additional (vehicle) group of mice receives water， while a further group of mice (untreated controls) are spared the aforementioned manipulations[2]. |
| 数据来源文献 |
[1]. Gutman DA， et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80.
[2]. Post A， et al. Identification of molecules potentially involved in mediating the in vivo actions of the corticotropin-releasing hormone receptor 1 antagonist， NBI30775 (R121919). Psychopharmacology (Berl). 2005 Jun;180(1):150-8.
[3]. Gutman DA， et al. Behavioral effects of the CRF1 recepator antagonist R121919 in rats selectively bred for high and low activity in the swim test. Psychoneuroendocrinology. 2008 Sep;33(8):1093-101. |
| 规格 |
1mg 5mg 10mg 25mg 50mg |
| 单位 |
瓶 |
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英语
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