Mosapride citrate

Names

[ Name ]:
Mosapride citrate

[Synonym ]:
5-Oxopentanoic acid - 4-amino-5-chloro-2-ethoxy-N-{[4-(4-fluorobe nzyl)-2-morpholinyl]methyl}benzamide (1:1)

Biological Activity

[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]:

Research Areas >> Metabolic Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

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

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

[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.

Chemical & Physical Properties

[ 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

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

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