Tegaserod maleate

Names

[ Name ]:
Tegaserod maleate

[Synonym ]:
(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)

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]:

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Research Areas >> Neurological Disease

[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.

[Related Small Molecules]

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

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

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%