Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C24H30ClFN4O4 |
| Molecular Weight | 492.971 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(C=C(Cl)C(N)=C1)C(=O)NCC2CCN(CC[C@H](OC(N)=O)C3=CC=C(F)C=C3)CC2
InChI
InChIKey=KGMMSPVVHZGPHL-NRFANRHFSA-N
InChI=1S/C24H30ClFN4O4/c1-33-22-13-20(27)19(25)12-18(22)23(31)29-14-15-6-9-30(10-7-15)11-8-21(34-24(28)32)16-2-4-17(26)5-3-16/h2-5,12-13,15,21H,6-11,14,27H2,1H3,(H2,28,32)(H,29,31)/t21-/m0/s1
Relenopride (YKP-10811) is a serotonin 4 (5-HT4) receptor agonist that was developed for regulation of gastric motility. It improved antral contractions and accelerated gastric emptying in dogs and had no adverse effects. Phase II clinical trials have investigated the efficacy and safety of relenopride in patients with (chronic and functional) constipation and irritable bowel syndrome (IBD). Relenopride was reported to accelerate gastrointestinal motility and colonic transit and improve bowel functions in patients with functional constipation, compared with placebo.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Participation of 5-HT3, 5-HT4, and nicotinic receptors in the peristaltic reflex of guinea pig distal colon. | 1996 Nov |
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| Signal transduction pathways for serotonin as an intestinal secretagogue. | 1997 Oct |
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| Serotonin: a mediator of the brain-gut connection. | 2000 Oct |
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| Rationale for using serotonergic agents to treat irritable bowel syndrome. | 2005 Apr 1 |
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| The serotonin signaling system: from basic understanding to drug development for functional GI disorders. | 2007 Jan |
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| Influence of a new 5-HT4 receptor partial agonist, YKP10811, on visceral hypersensitivity in rats triggered by stress and inflammation. | 2014 Dec |
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NCI_THESAURUS |
C47794
Created by
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C152177
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9919
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CD-75
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DB12798
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45275554
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1221416-43-8
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300000034311
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DTXSID50153530
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SIS5BFO4WL
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CHEMBL3544975
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
