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636582-62-2

636582-62-2 structure
636582-62-2 structure
  • Name: Mosapride citrate
  • Chemical Name: Mosapride Citrate Dihydrate
  • CAS Number: 636582-62-2
  • Molecular Formula: C26H33ClFN3O6
  • Molecular Weight: 538.00800
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2016-09-13 01:06:04
  • Modify Date: 2024-01-02 21:04:25
  • Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM[1]. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo[2].

Name Mosapride Citrate Dihydrate
Synonyms 5-Oxopentanoic acid - 4-amino-5-chloro-2-ethoxy-N-{[4-(4-fluorobe nzyl)-2-morpholinyl]methyl}benzamide (1:1)
Description Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM[1]. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo[2].
Related Catalog
Target

5-HT4 Receptor

Kv4.3:15.2 μM (IC50)

In Vitro Mosapride (0.3-30 μM) exhibits an inhibitory activity against Kv4.3 with an IC50 of 15.2 μM in a concentration-dependent manner. Mosapride also inhibits the open state of Kv4.3 currents during depolarization and accelerates the closed-state inactivation at subthreshold potentials[1].
In Vivo Mosapride (Intravenous injection;0.3-3 mg/kg) dose-dependently increases the antral motor activity in conscious dogs which indicates that mosapride selectively stimulates upper gastrointestinal motility[2]. Animal Model: Beagle dogs[2] Dosage: 0.3-3 mg/kg Administration: Intravenous injection; 0.3-3 mg/kg Result: Increased the antral motor activity dose-dependently in conscious dogs.
References

[1]. Sung KW, et al. Effect of mosapride on Kv4.3 potassium channels expressed in CHO cells. Naunyn-Schmiedeberg's archives of pharmacology. 2013;386(10):905-16.

[2]. Mine Y, et al. Comparison of effect of mosapride citrate and existing 5-HT4 receptor agonists on gastrointestinal motility in vivo and in vitro. The Journal of pharmacology and experimental therapeutics. 1997;283(3):1000-8.

Melting Point 112-114°C
Molecular Formula C26H33ClFN3O6
Molecular Weight 538.00800
Exact Mass 537.20400
PSA 134.68000
LogP 4.62490
Storage condition 2-8°C
Symbol GHS05
GHS05
Signal Word Danger
Hazard Statements H318
Precautionary Statements P280-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xi
Risk Phrases 41
Safety Phrases 26
RIDADR NONH for all modes of transport
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