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189188-57-6

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189188-57-6 Usage

Description

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).

Chemical Properties

White Powder

Originator

Novartis (Switzerland)

Uses

Different sources of media describe the Uses of 189188-57-6 differently. You can refer to the following data:
1. Tegaserod maleate has been used to study its cytotoxic effects on human astrocytes and to study its effects as an anti-glioblastoma agent.
2. Tegaserod is a gastroproeinetic used in the treatment of irritable bowel syndrome. A selective serotonin 5HT4-receptor partial agonist.

Brand name

Zelnorm (Novartis);Zelmac.

Biochem/physiol Actions

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.

Check Digit Verification of cas no

The CAS Registry Mumber 189188-57-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,8,9,1,8 and 8 respectively; the second part has 2 digits, 5 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 189188-57:
(8*1)+(7*8)+(6*9)+(5*1)+(4*8)+(3*8)+(2*5)+(1*7)=196
196 % 10 = 6
So 189188-57-6 is a valid CAS Registry Number.
InChI:InChI=1/C16H23N5O.C4H4O4/c1-3-4-5-8-18-16(17)21-20-11-12-10-19-15-7-6-13(22-2)9-14(12)15;5-3(6)1-2-4(7)8/h6-7,9-11,19H,3-5,8H2,1-2H3,(H3,17,18,21);1-2H,(H,5,6)(H,7,8)/b20-11+;2-1-

189188-57-6 Well-known Company Product Price

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  • Sigma

  • (SML1504)  Tegaserod maleate  ≥98% (HPLC)

  • 189188-57-6

  • SML1504-10MG

  • 1,107.99CNY

  • Detail
  • Sigma

  • (SML1504)  Tegaserod maleate  ≥98% (HPLC)

  • 189188-57-6

  • SML1504-50MG

  • 4,469.40CNY

  • Detail

189188-57-6SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 18, 2017

Revision Date: Aug 18, 2017

1.Identification

1.1 GHS Product identifier

Product name tegaserod maleate

1.2 Other means of identification

Product number -
Other names Tegaserod Maleate

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:189188-57-6 SDS

189188-57-6Synthetic route

2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide D-(+)-camphorsulphonate

2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide D-(+)-camphorsulphonate

maleic acid
110-16-7

maleic acid

tegaserod maleate
189188-57-6

tegaserod maleate

Conditions
ConditionsYield
In dichloromethane; water at 30 - 35℃; for 1h;90%
maleic acid
110-16-7

maleic acid

tegaserod
145158-71-0

tegaserod

tegaserod maleate
189188-57-6

tegaserod maleate

Conditions
ConditionsYield
In butanone at 25 - 44℃; for 0.5 - 1h; Purification / work up;70.2%
In methanol at 25℃; for 0.5h;
In methanol; dichloromethane at 25℃; for 1h; Heating / reflux;
In methanol; isopropyl alcohol at 25℃; for 1h;

189188-57-6Downstream Products

189188-57-6Relevant articles and documents

New tegaserod maleate polymorphs and process for their preparation

-

Page/Page column 4, (2008/12/07)

The present invention refers to two new tegaserod maleate polymorfs (α and β) and to processes for their preparation.

NOVEL CRYSTALLINE FORMS OF TEGASEROD MALEATE

-

Page 4, (2008/06/13)

The present invention relates to novel crystalline forms to tegaserod maleate, to processes for their preparation and to pharmaceutical compositions containing them.

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