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).
Tegaserod is a gastroproeinetic used in the treatment of irritable bowel syndrome. A selective serotonin 5HT4-receptor partial agonist.
Tegaserod maleate has been used to study its cytotoxic effects on human astrocytes and to study its effects as an anti-glioblastoma agent.
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.
