Itopride

Modify Date: 2024-01-02 15:14:54

Itopride Structure
Itopride structure
Common Name Itopride
CAS Number 122898-67-3 Molecular Weight 358.431
Density 1.1±0.1 g/cm3 Boiling Point 510.1±50.0 °C at 760 mmHg
Molecular Formula C20H26N2O4 Melting Point 185-187 °C(lit.)
MSDS N/A Flash Point 262.3±30.1 °C

 Use of Itopride


Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD)[1].

 Names

Name N-[[4-[2-(dimethylamino)ethoxy]phenyl]methyl]-3,4-dimethoxybenzamide
Synonym More Synonyms

 Itopride Biological Activity

Description Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD)[1].
Related Catalog
Target

D2 Receptor

Acetylcholinesterase

In Vitro Itopride has prokinetic effects on both the ileum and colon, which are regulated through inhibitory effects on AChE and antagonistic effects on dopamine D2 receptor[3]. Itopride hydrochloride (0.1 nM-1 μM) significantly accelerats the propagation velocity of the peristalsis in ex guinea pig ileum[3].
In Vivo Itopride (30 mg/kg; p.o.) significantly accelerates gastric emptying compared with the vehicle group[4]. Itopride (30 mg/kg; p.o.) displays Cmax of 358 ‰, T1/2 of 24.9 min[4].
References

[1]. Iwanaga Y, et al. A novel water-soluble dopamine-2 antagonist with anticholinesterase activity in gastrointestinal motor activity. Comparison with domperidone and neostigmine. Gastroenterology. 1990 Aug;99(2):401-8.

[2]. Kim YS, et al. Effect of itopride, a new prokinetic, in patients with mild GERD: a pilot study. World J Gastroenterol. 2005 Jul 21;11(27):4210-4.

[3]. Hyun Chul Lim, et al. Effect of Itopride Hydrochloride on the Ileal and Colonic Motility in Guinea Pig In Vitro. Effect of Itopride Hydrochloride on the Ileal and Colonic Motility in Guinea Pig In Vitro. Yonsei Med J. 2008 Jun 30;49(3):472-8.

[4]. Kenjiro Matsumoto, et al. Validation of 13 C-Acetic Acid Breath Test by Measuring Effects of Loperamide, Morphine, Mosapride, and Itopride on Gastric Emptying in Mice. Biol Pharm Bull. 2008 Oct;31(10):1917-22.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 510.1±50.0 °C at 760 mmHg
Melting Point 185-187 °C(lit.)
Molecular Formula C20H26N2O4
Molecular Weight 358.431
Flash Point 262.3±30.1 °C
Exact Mass 358.189270
PSA 60.03000
LogP 2.43
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.552
Water Solubility 18 g/100 mL (20 ºC)

 Customs

HS Code 2924299090
Summary 2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

 Synonyms

MFCD00867431
Itopride
Itopride (INN)
UNII-81BMQ80QRL
N-<4-<2-(dimethylamino)ethoxy>benzyl>-3,4-dimethoxybenzamide
Benzamide, N-[[4-[2-(dimethylamino)ethoxy]phenyl]methyl]-3,4-dimethoxy-
Ganaton
[125I]-Itopride
N-{4-[2-(Dimethylamino)ethoxy]benzyl}-3,4-dimethoxybenzamide
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