| 产品描述: | WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM |
| 靶点: |
IC50: 2.3 nM (ERRβ), 155 nM (ERRα);EstrogenReceptor/ERR;Estrogen/progestogenReceptor |
| 体外研究: |
Administration of WAY-200070 (30 mg/kg s.c.) causes nuclear translocation of ERRβ receptors in WT mice. Administration of WAY-200070 (30 mg/kg s.c.) produces a delayed 50% increase in dopamine in the striatum of wild type mice. WAY-200070 (30 mg/kg s.c.) reduces immobility time in the mouse tail suspension test indicating an antidepressant-like effect. In gonadally intact male and female mice WAY-200070 increases agonistic behaviors such as pushing down and aggressive grooming, while leaving attacks unaffected. Ovariectomized (ovx) mice treated with PPT fail to learn the socially acquired preference, while WAY-200070-treated ovx mice shows a two-fold prolonged preference for the food eaten by their demonstrator. WAY-200070, shows significantly decreased anxiety-like behaviors in both the open-field and elevated plus maze and significantly less depressive-like behaviors in the forced swim test |
| 体内研究: |
施用 WAY-200070 (30 mg/kg sc) 导致 WT 小鼠中 ERRβ 受体的核转位。施用 WAY-200070 (30 mg/kg sc) 会使野生型小鼠纹状体中的多巴胺延迟增加 50%。WAY-200070 (30 mg/kg 皮下注射) 减少了小鼠悬尾试验中的不动时间,表明具有抗抑郁样作用。 在性腺完整的雄性和雌性小鼠中,WAY-200070 会增加竞争行为,例如向下推和攻击性梳理毛发,同时不影响攻击。 用 PPT 处理的卵巢切除 (ovx) 小鼠无法学习社会获得的偏好,而 WAY-200070 处理的 ovx 小鼠显示对其示范者所吃食物的偏好延长两倍。 WAY-200070 显示在开放场和高架十字迷宫中的焦虑样行为显著减少,在强迫游泳测试中的抑郁样行为显著减少。 |
| 参考文献: |
1. Hughes ZA, et al. WAY-200070, a selective agonist of estrogen receptor beta as a potential novel anxiolytic/antidepressant agent. Neuropharmacology. 2008 Jun;54(7):1136-42. 2. Clipperton Allen AE, et al. Agonistic behavior in males and females: effects of an estrogen receptor beta agonist in gonadectomized and gonadally intact mice. Psychoneuroendocrinology. 2010 Aug;35(7):1008-22. 3. Clipperton AE, et al. Differential effects of estrogen receptor alpha and beta specific agonists on social learning of food preferences in female mice. Neuropsychopharmacology. 2008 Sep;33(10):2362-75. 4. Weiser MJ, et al. Estrogen receptor-beta agonist diarylpropionitrile: biological activities of R- and S-enantiomers on behavior and hormonal response to stress. Endocrinology. 2009 Apr;150(4):1817-25. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.267 ml |
16.334 ml |
32.668 ml |
| 5 mM |
0.653 ml |
3.267 ml |
6.534 ml |
| 10 mM |
0.327 ml |
1.633 ml |
3.267 ml |
| 50 mM |
0.065 ml |
0.327 ml |
0.653 ml |
|
| 注意: |
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