A 5-HT4 receptor agonist (IC50 = 0.483 μM in COS-7 cells expressing the human receptor); induces relaxation of precontracted isolated rat esophageal thoracic muscularis mucosae preparations (EC50 = 102.33 nM); increases the rate of gastric emptying in rats at (0.5 mg/kg); an hERG channel blocker; bind to hERG channels (IC50 =

Cisapride – 50 mg

Brand:
Cayman
CAS:
81098-60-4
Storage:
-20
UN-No:
Non-Hazardous - /

Cisapride is an agonist of serotonin (5-HT) receptor subtype 5-HT4 (IC50 = 0.483 μM in COS-7 cells expressing the human receptor).{34540} It induces relaxation of precontracted isolated rat esophageal thoracic muscularis mucosae preparations (EC50 = 102.33 nM). Cisapride (0.5 mg/kg) increases the rate of gastric emptying in rats. It is also a human ether-a-go-go related gene (hERG) channel blocker that binds to hERG channels with an IC50 value of less than 1 μM in a fluorescence polarization assay. Formulations containing cisapride have previously been used in the treatment of nocturnal heartburn associated with gastroesophageal reflux disease.  

 

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Description

A 5-HT4 receptor agonist (IC50 = 0.483 μM in COS-7 cells expressing the human receptor); induces relaxation of precontracted isolated rat esophageal thoracic muscularis mucosae preparations (EC50 = 102.33 nM); increases the rate of gastric emptying in rats at (0.5 mg/kg); an hERG channel blocker; bind to hERG channels (IC50 = <1 μM in a fluorescence polarization assay)

Formal name: rel-4-amino-5-chloro-N-[1-[(3R,4S)-3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxy-benzamide

Synonyms: 

Molecular weight: 466

CAS: 81098-60-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Gastric Disease

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