SR 57227A ≥98%
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| 包装规格: | 1mg 5mg 10mg 25mg 50mg 100mg in glass bottle |
| 溶解性: | 溶于DMSO(8.33mg/mL 超声) |
| 产品描述: | 基本信息 产品编号: S10813 产品名称: SR 57227A CAS: 77145-61-0 储存条件 粉末 2-8℃ 四年 分子式: C10H15Cl2N3 溶于液体 -80℃ 6个月 分子量 248.15 -20℃ 1个月 化学名: 1-(6-chloropyridin-2-yl)piperidin-4-amine,hydrochloride Solubility (25°C): 体外: DMSO 5 mg/mL (20.15mM; Need ultrasonic) Ethanol Water 33.33 mg/mL (134.31mM; Need ultrasonic) 体内(现配现用): <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 生物活性 产品描述 一种具有口服活性的 5-HT3 受体的一种选择性激动剂, 可透过血脑屏障。SR 57227A 对大鼠皮质膜和整个 NG 108-15 细胞或其膜上 5-HT3 受体结合位点的亲和力 (IC50) 在 2.8~250nM。具有抗抑郁作用。 靶点 5-HT Receptor 体外研究 SR 57227A binds to 5-HT3 receptors labelled with [3H]S-zacopride with an affinity (Ki ) of 115nM in rat cerebral cortex, 150nM in NG 108-15 cell membranes and 103nM in whole NG 108-15 cell. 体内研究 SR 57227A (1-30 mg/kg; i.p.) dose-dependently reduces immobility time in the forced swimming test with an ED50 value for this effect of 14.2 mg/kg. In the forced swimming test, SR 57227A dose-dependently reduces the duration of immobility in rats after i.p. administration. (ED50=7.6 mg/kg i.p. in rats.) SR 57227A is also active in both species after oral administration. In a timecourse study in mice, SR 57227A (20 mg/kg p.o.) produces a significant effect lasting 6 hours. SR 57227A (1 and 3 mg/kg i.p.) reduces the elevation of the escape failures in the learned helplessness model in rats by 50-60% on the last two days of the avoidance task, and reduces isolation-induced aggressivity in mice by 50 to 85%, an effect which is antagonised by Zacopride (1 mg/kg i.p.). |
| 保存条件: | 2-8℃ 干燥 |
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