Tegaserod maleate

Modify Date: 2024-01-02 16:39:56

Tegaserod maleate Structure
Tegaserod maleate structure
 Common Name Tegaserod maleate
CAS Number 189188-57-6 Molecular Weight 417.459
Density N/A Boiling Point 661.4ºC at 760 mmHg
Molecular Formula C20H27N5O5 Melting Point 180-183ºC
MSDS Chinese USA Flash Point 353.8ºC

 Use of Tegaserod maleate


Tegaserod maleate is a partial agonist of the 5-HT4 receptor; stimulates the peristaltic reflex and accelerates gastrointestinal transit.IC50 value:Target: 5-HT4 agonistIn an in vivo model for peripheral nerve regeneration, mice receiving tegaserod at the site of injury showed enhanced recovery compared to control mice receiving vehicle control as evidenced by functional measurements and histology [1]. Treatment with fluoxetine (10 mg · kg(-1) · day(-1), days 36-42), tegaserod (1 mg · kg(-1) · day(-1), day 43), or the combination of both, reduced visceral hypersensitivity and plasma 5-HT levels [2]. Intravenous or intraduodenal tegaserod (0.3-1.0 mg.kg(-1)) had no inhibitory effect on mesenteric and colonic blood flow. Peroral treatment of rats with alosetron or tegaserod for 7 days did not modify mesenteric haemodynamics at baseline and after blockade of nitric oxide synthesis [3].

 Names

Name tegaserod maleate
Synonym More Synonyms

 Tegaserod maleate Biological Activity

Description Tegaserod maleate is a partial agonist of the 5-HT4 receptor; stimulates the peristaltic reflex and accelerates gastrointestinal transit.IC50 value:Target: 5-HT4 agonistIn an in vivo model for peripheral nerve regeneration, mice receiving tegaserod at the site of injury showed enhanced recovery compared to control mice receiving vehicle control as evidenced by functional measurements and histology [1]. Treatment with fluoxetine (10 mg · kg(-1) · day(-1), days 36-42), tegaserod (1 mg · kg(-1) · day(-1), day 43), or the combination of both, reduced visceral hypersensitivity and plasma 5-HT levels [2]. Intravenous or intraduodenal tegaserod (0.3-1.0 mg.kg(-1)) had no inhibitory effect on mesenteric and colonic blood flow. Peroral treatment of rats with alosetron or tegaserod for 7 days did not modify mesenteric haemodynamics at baseline and after blockade of nitric oxide synthesis [3].
Related Catalog
References

[1]. Bushman J, et al. Tegaserod mimics the neurostimulatory glycan polysialic acid and promotes nervous system repair. Neuropharmacology. 2014 Apr;79:456-66.

[2]. Yan C, et al. Effect of the 5-HT4 receptor and serotonin transporter on visceral hypersensitivity in rats. Braz J Med Biol Res. 2012 Oct;45(10):948-54.

[3]. Painsipp E, et al. Alosetron, cilansetron and tegaserod modify mesenteric but not colonic blood flow in rats. Br J Pharmacol. 2009 Nov;158(5):1210-26.

 Chemical & Physical Properties

Boiling Point 661.4ºC at 760 mmHg
Melting Point 180-183ºC
Molecular Formula C20H27N5O5
Molecular Weight 417.459
Flash Point 353.8ºC
Exact Mass 417.201233
PSA 149.45000
LogP 3.10190
Vapour Pressure 2.15E-18mmHg at 25°C
Storage condition -20°C Freezer

 Safety Information

RIDADR NONH for all modes of transport
HS Code 2933990090

 Synthetic Route

Maleic acid structure

Maleic acid

CAS#:110-16-7

Tegaserod structure

Tegaserod

CAS#:145158-71-0

~72%

Tegaserod maleate Structure

Tegaserod maleate

CAS#:189188-57-6

Literature: Venkataraman, Sundaram; Gudipati, Srinivasulu; Mandava Venkata Naga, Brahmeshwararao; Banda, Goverdhan Reddy; Singamsetty, Radhakrishna Patent: US2005/272802 A1, 2005 ; Location in patent: Page/Page column 2-3 ;

 Precursor & DownStream

Precursor  2

DownStream  0

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

(2E)-2-[(5-Methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide (2Z)-2-butenedioate
Zelnorm
Hydrazinecarboximidamide, 2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentyl-, (2E)-, (2Z)-2-butenedioate (1:1)
(2E)-2-[(5-methoxy-1H-indol-3-yl)methylidene]-N-pentylhydrazinecarboximidamide (2Z)-but-2-enedioate (1:1)
Zelmac
MFCD04116201
acide (2Z)-but-2-ènedioïque - (2E)-2-[(5-méthoxy-1H-indol-3-yl)méthylidène]-N-pentylhydrazinecarboximidamide (1:1)
Tegaserod Maleate
(2E)-2-[(5-Methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide (2Z)-but-2-enedioate (1:1)
(2Z)-But-2-endisäure--(2E)-2-[(5-methoxy-1H-indol-3-yl)methyliden]-N-pentylhydrazincarboximidamid(1:1)
(2E)-2-[(5-Methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide (2Z)-2-butenedioate (1:1)
(2E)-2-[(5-methoxy-1H-indol-3-yl)methylidene]-N-pentylhydrazinecarboximidamide (2Z)-but-2-enedioate
Tegaserod (maleate)
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