1184662-54-1
Chemical Structure
Minesapride
Synonym(s): DSP-6952 free base
- CAS No.: 1184662-54-1
- Formula:C21H31ClN4O5
- Molecular Weight:454.95
IUPAC Name: (S)-4-amino-5-chloro-N-((4-((1-(2-hydroxyacetyl)piperidin-4-yl)methyl)morpholin-2-yl)methyl)-2-methoxybenzamide
InChIKey: YNGWOFISMAAXPB-HNNXBMFYSA-N
SMILES: OCC(N(CC1)CCC1CN(CCO2)C[C@@H]2CNC(C3=C(C=C(C(Cl)=C3)N)OC)=O)=O
Biological Activity: Minesapride (DSP-6952 free base) is an orally active, selective 5-HT4 receptor partial agonist. Minesapride enhances gastrointestinal motility, colonic transit and defecation function, and inhibits visceral hypersensitivity. Minesapride does not inhibit/induce cytochrome P450 isozymes, has no significant affinity for hERG, and does not trigger the risk of cardiac ischemia via coronary vasoconstriction. Minesapride can be used in research related to constipation-predominant irritable bowel syndrome, chronic constipation, atonic constipation, spastic constipation, functional constipation and functional dyspepsia[1][2][3][4].
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Minesapride | Minesapride (DSP-6952 free base) is an orally active, selective 5-HT4 receptor partial agonist. Minesapride enhances gastrointestinal motility, colonic transit and defecation function, and inhibits visceral hypersensitivity. Minesapride does not inhibit/induce cytochrome P450 isozymes, has no significant affinity for hERG, and does not trigger the risk of cardiac ischemia via coronary vasoconstriction. Minesapride can be used in research related to constipation-predominant irritable bowel syndrome, chronic constipation, atonic constipation, spastic constipation, functional constipation and functional dyspepsia. | |||||||||||||||||||||
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References
- [1]. Fukudo S, et al. Efficacy and Safety of 5-HT4 Receptor Agonist Minesapride for Irritable Bowel Syndrome with Constipation in a Randomized Controlled Trial. Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association. 2021 Mar;19(3):538-546.e8. [Content Brief]
- [2]. Mine Y, et al. DSP-6952, a novel 5-HT receptor partial agonist, inhibits visceral hypersensitivity and ameliorates gastrointestinal dysfunction in experimental animals. European journal of pharmacology. 2018 May 05;826:123-132.
- [3]. Hamatani T, et al. Pharmacokinetics, safety and metabolite profiling of minesapride, a novel 5-HT receptor partial agonist, in healthy elderly and young subjects. Drug metabolism and pharmacokinetics. 2020 Dec;35(6):563-570.
- [4]. Tsubouchi T, et al. The in vitro pharmacology and non-clinical cardiovascular safety studies of a novel 5-HT receptor agonist, DSP-6952. European journal of pharmacology. 2018 May 05;826:96-105.
