SR 57227A

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SR 57227A

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

77145-61-0

SR 57227A 是具有口服活性的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 2.8~250 nM。具有抗抑郁作用。

生物活性

SR 57227A is a potent, orally active and selective5-HT3 receptoragonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC₅₀) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects^[1]^[2].

体外研究
(In Vitro)

SR 57227A binds to 5-HT3 receptors labelled with [3H]S-zacopride with an affinity (K_i) of 115 nM in rat cerebral cortex, 150 nM in NG 108-15 cell membranes and 103 nM in whole NG 108-15 cell^[1].

体内研究
(In Vivo)

SR 57227A (1-30 mg/kg; i.p.) dose-dependently reduces immobility time in the forced swimming test with an ED₅₀value for this effect of 14.2 mg/kg^[2].
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 time-course 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.)^[2].

分子量

248.15

性状

Solid

Formula

C₁₀H₁₅Cl₂N₃

CAS 号

77145-61-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 33.33 mg/mL(134.31 mM;Need ultrasonic)

DMSO : 8.33 mg/mL(33.57 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	4.0298 mL	20.1491 mL	40.2982 mL
5 mM	0.8060 mL	4.0298 mL	8.0596 mL
10 mM	0.4030 mL	2.0149 mL	4.0298 mL

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。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 10 mg/mL (40.30 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

*以上所有助溶剂都可在本网站选购。