Mosapride citrate (Gasmotin citrate) is a synthetic, agonist of the 5-HT4 receptor with an IC50 of 113 nM and an antagonist of the 5-HT3 receptor and does not show significant activity at other 5-HT receptors. Mosapride has an effective concentration of 5-500 μM. Mosapride substantially enhances GI motility by stimulating 5-HT4 receptors in dogs. This effect is long lasting and mostly occurs in the animal’s upper GI and not in the colon. This is contrary to other gastro prokinetic drugs such as cisapride and zacopride that have a shorter half-life and a combined effect. in vitro, Mosapride is only a partial agonist of 5-HT receptors located in guinea pig distal colon and terminal ileum tissues. In addition Mosapride causes a relaxation in rat thoracic esophageal muscularis mucosae treated with carbachol. In view of its different activity along the gut, Mosapride can be used to demonstrate and explore the existence of different types of 5-HT4 receptors in the GI.
产品描述
An Antagonist of 5-HT3 Receptors and an Agonist of 5-HT4 Receptors
产品形式
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid Tryptophan by the enzyme tryptophan-decarboxylase. The 5-HT3 channel is a ligand gated ion channel receptor of the cys-loop channel family. It is a pentamer with five subunits surrounding a central channel.
