| 名称 | Prucalopride |
| 描述 | Prucalopride (R-93877) is a selective, high-affinity 5-HT4A/4B receptor agonist (Ki: 2.5/8 nM). It has >290-fold selectivity for 5-HT4A/4B receptor than other 5-HT receptor subtypes. |
| 体外活性 | Administration of prucalopride at dosages of 2/4 mg resulted in complete spontaneous bowel movements per week at rates of 30.9% and 28.4%, respectively, compared to 12.0% in the placebo group. Patients treated with 2 mg of prucalopride (47.3%) and those receiving 4 mg (46.6%) experienced an increase in the frequency of spontaneous bowel movements, with an average of one or more complete bowel movements per week, versus 25.8% in the placebo group. Prucalopride (2/4 mg) significantly enhanced other secondary efficacy endpoints, including patient satisfaction with their bowel functions and treatment, as well as their perception of the severity of constipation symptoms. At a dosage of 4 mg/day, prucalopride accelerated overall gastric emptying and small intestinal transit without causing intestinal evacuation disorders. It also sped up overall colonic transit and increased the colonic emptying rate. |
| 体内活性 | Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea pig's proximal colon following electrical stimulation. It induces contractions in a concentration-dependent manner (pEC50: 7.5). Additionally, Prucalopride induces relaxation in the muscularis mucosae of the rat esophagus (pEC50: 7.8), demonstrating a monophasic concentration-response curve. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 36 mg/mL (97.9 mM)
DMSO : 56 mg/mL (152.2 mM)
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| 关键字 | Serotonin Receptor | A549 | 5-hydroxytryptamine Receptor | chronic constipation | pseudo-intestinal obstruction | inhibit | 5-HT Receptor | Prucalopride | R 93877 | A427 | Inhibitor | R93877 | Lung cancer |
| 相关产品 | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| 相关库 | 神经退行性疾病化合物库 | 疼痛相关化合物库 | 经典已知活性库 | 膜蛋白靶向化合物库 | EMA 上市药物库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | FDA 上市药物库 | 已知活性化合物库 | GPCR靶点分子库 |
United States
