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Cisapride

CAS No. : 81098-60-4

MCE 国际站：Cisapride

产品活性：Cisapride (R 51619) 是一种具有口服活性的的 5-HT₄ 受体激动剂，EC₅₀ 值为 140 nM。Cisapride 是 hERG 阻断剂，IC₅₀ 值为 9.4 nM。Cisapride 是一种胃促动力剂，可刺激胃肠运动活动。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Membrane Transporter/Ion Channel

作用靶点：5-HT Receptor  |  Potassium Channel

In Vitro: Cisapride (1-100 nM) is a potent hERG blockers with an IC₅₀ value of 9.4 nM.
Cisapride (1-100 nM) shows efficacy to 5-HT₄ receptor with an EC₅₀ value of 140 nM.
Cisapride (0.3, 1, 3, 10 and 30 μM) dose-dependently inhibits Kv4.3 with an IC₅₀ value of 9.8 μM in Kv4.3 potassium channels expressing CHO cells.

In Vivo: Cisapride (0.1-1 mg/kg; i.v., once) stimulates antral and colonic motility in conscious dogs.
Cisapride (2 mg/kg (i.p.); 4 mg/kg, (oral administration); once) shows no significant differences in macroscopic features, histopathological features, cytokines profile and bodyweight changes with TNBS-treated rats.

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