A 5-HT4 receptor agonist
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Metabolite(s)
22157Des-4-fluorobenzyl Mosapride
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Mosapride (citrate)

Item No. 30048

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]-2-morpholinyl]methyl]-benzamide, 2-hydroxy-1,2,3-monopropanetricarboxylate
CAS Number
112885-42-4
Synonyms
  • AS-4370
Molecular Formula
C21H25ClFN3O3 • C6H8O7
Formula Weight
614.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 15 mg/ml
λmax
212, 232, 274, 309 nm
SMILES
ClC1=C(N)C=C(OCC)C(C(NCC2OCCN(CC3=CC=C(F)C=C3)C2)=O)=C1.OC(CC(C(O)=O)(O)CC(O)=O)=O
InChi Code
InChI=1S/C21H25ClFN3O3.C6H8O7/c1-2-28-20-10-19(24)18(22)9-17(20)21(27)25-11-16-13-26(7-8-29-16)12-14-3-5-15(23)6-4-14;7-3(8)1-6(13,5(11)12)2-4(9)10/h3-6,9-10,16H,2,7-8,11-13,24H2,1H3,(H,25,27);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)
InChi Key
HUZTYZBFZKRPFG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

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    50 mg

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    100 mg

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    250 mg

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    Product Description

    Mosapride is an agonist of the serotonin (5-HT) receptor subtype 5-HT4 (Ki = 69.9 nM).1,2 It is selective for 5-HT4 over 5-HT1, 5-HT2, dopamine D2, and α1- and α2-adrenergic receptors but acts as a partial antagonist at 5-HT3 (Ki = 1,189 nM).1,2 It induces relaxation of precontracted rat esophageal thoracic muscularis mucosa preparations and enhances electrically evoked contractions in isolated guinea pig ileum (EC50s = 208.4 and 73.2 nM, respectively).3 Mosapride (0.5 and 1 mg/kg, i.v.) increases antral and duodenal, but not ileal or colonic, motility in conscious dogs.1 It also increases gastric emptying in rats when administered at doses ranging from 0.03 to 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yoshida, N., Omoya, H., Oka, M., et al. AS-4370, a novel gastrokinetic agent free of dopamine D2 receptor antagonist properties. Arch. Int. Pharmacodyn. Ther. 300, 51-67 (1989).

    2. Hirokawa, Y., Fujiwara, I., Suzuki, K., et al. Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity. J. Med. Chem. 46(5), 702-715 (2003).

    3. Mine, Y., Yoshikawa, T., Oku, S., et al. Comparison of effect of mosapride citrate and existing 5-HT4 receptor agonists on gastrointestinal motility in vivo and in vitro. J. Pharmacol. Exp. Ther. 283(3), 1000-1008 (1997).