cisapride

Cisapride (R 51619) 是一种5-HT4受体激动剂，还是 hERG 抑制剂。它可作用于肠道中的血清素受体，促进肠道蠕动，增加胃排空并减少食管反流。

Cisapride tartrate is chemically related to metoclopramide, but unlike metoclopramide, it does not cross the blood-brain barrier or have antidopaminergic effects. Cisapride is a serotonin-4 (5-HT4) receptor agonist. Cisapride was indicated for the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. The Food and Drug Administration (FDA) in America stopped the marketing of cisapride as of 14th July 2000. They had received at least 341 reports of heart rhythm abnormalities and these led to 80 deaths. Other reported adverse effects are: headache, diarrhea, abdominal pain, nausea, constipation. Cisapride for animals has been found helpful in some cases of megaesophagus and is a common treatment for feline megacolon. Clarithromycin, erythromycin, and troleandomycin markedly inhibit the metabolism of cisapride. Concurrent administration of certain anticholinergic compounds, such as belladonna alkaloids and dicyclomine, would be e......

Cisapride acts directly as a selective agonist of serotonin 5-HT4 receptor with IC50 value of 0.483 μM. And It also acts indirectly as a parasympathomimetic.

Norcisapride 是一种5-羟色胺受体3（5-HT3）和(5-羟色胺受体4（5-HT4） 双重激动剂，可用于治疗消化系统疾病、口颌疾病和耳鼻咽喉疾病。

Norcisapride 属于被称为二苯基吡咯的一类有机化合物。Norcisapride 直接作为5-羟色胺5-HT4受体激动剂发挥作用，并间接作为拟副交感神经发挥作用。Norcisapride 是 Cisapride 的代谢产物。

R 50595 is a selective non-competitive cisapride antagonist.