产品
编 号:F467060
分子式:C23H29ClFN3O4
分子量:465.95
产品类型
结构图
CAS No: 81098-60-4
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生物活性:
Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity.
体内研究:
Cisapride (0.1-1 mg/kg;静脉注射,一次) 刺激清醒犬的胃窦和结肠运动。Cisapride (2 mg/kg,(腹腔注射);4 mg/kg,(口服);一次)与三硝基苯磺酸处理的大鼠在宏观特征、组织病理学特征、细胞因子谱和体重变化均无显著差异。Animal Model:Male Wistar rats with trinitrobenzenesulfonic-acid-(TNBS) induced rat colitis
Dosage:2 mg/kg (i.p.); 4 mg/kg, (oral administration)
Administration:2 mg/kg, intraperitoneal injection ; 4 mg/kg, oral administration; once
Result:Showed severe and intense transmural inflammation and diffuse necrosis, inflammatory granulomas and submucosal neutrophils infiltration in colitis rat. Induced body weight loss.
体外研究:
Cisapride (1-100 nM) 是一种有效的 hERG 阻断剂,IC50 值为 9.4 nM。Cisapride (1-100 nM) 对 5-HT4 受体有效,EC50 值为 140 nM。Cisapride (0.3,1,3,10 和 30 μM) 对 Kv4.3 的抑制作用呈剂量依赖性,IC50 值为 9.8 μM 在表达 Kv4.3 钾通道的 CHO 细胞。