189188-57-6

Tegaserod maleate was launched as a new oral treatment of constipationpredominant or diarrhea-predominant irritable bowel syndrome. It can be prepared by condensation of the 5-methoxy-3-formylindole with the appropriate aminoguanidine. Tegaserod is a selective partial agonist of the excitatory 5-HT₄ receptor (K₁ = 18 nM in human caudate membranes) and was designed from the endogenous full agonist, seretonin. In the model of potentiation of the electrically stimulated contraction of longitudinal muscle of guinea pig ileum, Tegaserod exhibited a low-efficacy agonistic activity compared with serotonin. However, it appeared more potent in several studies on intestinal mucosal tissue from various species including man. A lack of effect on the QTc interval was shown in rabbits then confirmed during clinical studies. Tegaserod is also clinically developed for the treatment of other functional GI disorders such as functional dyspepsia and gastroesophageal reflux disease (GERD).

White Powder

Novartis (Switzerland)

Tegaserod is a gastroproeinetic used in the treatment of irritable bowel syndrome. A selective serotonin 5HT4-receptor partial agonist.

Zelnorm (Novartis);Zelmac.

It stimulates neurotransmitter release from enteric nerves and regularizes gastrointestinal function. Tegaserod has been used to treat irritable bowel syndrome associated with constipation and chronic constipation.

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