Bioactivity | 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]. |
Invitro | 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: |
Name | Mosapride citrate dihydrate |
CAS | 636582-62-2 |
Formula | C27H37ClFN3O12 |
Molar Mass | 650.05 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |