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SR 57227A

CAS No. : 77145-61-0

MCE 站：SR 57227A

产品活性：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。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

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.

In Vivo: 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 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.).

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