Mosapride citrate

Gasmotin citrate, TAK-370 citrate, AS-4370 citrate
An Antagonist of 5-HT3 Receptors and an Agonist of 5-HT4 Receptors
    Cat #: M-225
    Alternative Name Gasmotin citrate, TAK-370 citrate, AS-4370 citrate
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 614
    Purity: >99%
    Effective concentration 5-500 µM.
      • Mosapride citrate
    Chemical name 4-amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl]benzamide;2-hydroxypropane-1,2,3-tricarboxylic acid.
    Molecular formula C27H33ClFN3O10.
    CAS No.: 112885-42-4.
    PubChem CID 119583
    Activity Mosapride citrate is a 5-HT4 receptor agonist and 5-HT3 receptor antagonist1.
      • Mine, Y. et al. (1997) J. Pharmacol. Exp. Ther. 283, 1000.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
      • Mosapride citrate
        Alomone Labs Mosapride citrate blocks 5-HT3A receptors expressed in HEK 293T cells. 
        5-HT3A receptor currents were elicited with 10 µM 5-HT, delivered every 3 minutes. Mosapride citrate (#M-225) was applied 30 seconds before stimulation at 50, 100 and 330 µM as indicated and inhibited the 5-HT induced current in a dose dependent and reversible manner.
    References - Scientific background
    • 1. Hannon, J. et al. (2008) Behav. Brain Res. 195, 198.
    • 2. Mine, Y. et al. (1997) J. Pharmacol. Exp. Ther. 283, 1000.
      • Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid Tryptophan by the enzyme tryptophan-decarboxylase. The 5-HT3 channel is a ligand-gated ion channel receptor of the cys-loop channel family. It is a pentamer with five subunits surrounding a central channel1.

        Mosapride citrate (Gasmotin citrate) is a synthetic, agonist of the 5-HT4 receptor with an IC50 of 113 nM and an antagonist of the 5-HT3 receptor and does not show significant activity at other 5-HT receptors. Mosapride has an effective concentration of 5-500 μM. Mosapride substantially enhances GI motility by stimulating 5-HT4 receptors in dogs. This effect is long lasting and mostly occurs in the animal’s upper GI and not in the colon. This is contrary to other gastro prokinetic drugs such as cisapride and zacopride that have a shorter half-life and a combined effect. in vitro, Mosapride is only a partial agonist of 5-HT receptors located in guinea pig distal colon and terminal ileum tissues. In addition, Mosapride causes a relaxation in rat thoracic esophageal muscularis mucosae treated with carbachol. In view of its different activity along the gut, Mosapride can be used to demonstrate and explore the existence of different types of 5-HT4 receptors in the GI2.

    Target 5-HT3 and 5-HT4 receptors
    Last update: 24/01/2020

    Mosapride citrate (#M-225) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use