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Open Access Articles- Top Results for Piboserod

Piboserod

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Piboserod
File:Piboserod.png
Systematic (IUPAC) name
N-((1-Butyl-4-piperidyl)-methyl)-3,4-dihydro-2H-(1,3)oxazino(3,2-a)indole-10-carboxamide
Clinical data
  • Clinical phase II
Oral
Identifiers
152811-62-6 7pxY
None
PubChem CID 177336
IUPHAR ligand 225
ChemSpider 154413 7pxN
UNII 4UQ3S81B25 7pxN
ChEMBL CHEMBL356359 7pxN
Chemical data
Formula C22H31N3O2
369.50 g/mol
 14pxN (what is this?)  (verify)

Piboserod is a selective 5-HT4 receptor antagonist which was marketed and manufactured by GlaxoSmithKline (GSK) under the trade name Serlipet for the management of atrial fibrillation and irritable bowel syndrome. In 2007 the Norwegian company Bio-Medisinsk Innovasjon AS (BMI)[1] completed a clinical phase II study to investigate the effect of piboserod in patients with chronic heart failure.

Mechanism of action

In 2002 a research group at the University of Oslo discovered that muscles from the ventricle of failing hearts have increased responsiveness to serotonin.[2] They later demonstrated that the effect was due to an expression of functional 5-HT4 receptors in the failing muscle. On the basis of these findings, and in analogy with the success of betablockers in heart failure, the group made the hypothesis that 5-HT4 receptor antagonists could be useful to treat heart failure. Their hypothesis was tested in animal models of heart failure with positive results.[3]

References

  1. ^ Company web-page
  2. ^ Bratteli T. et al., Functional serotonin 5-HT4 receptors in porcine and human ventricular myocardium with increased 5-HT4 mRNA in heart failure. Naunyn-Schmiedeberg's Arch. Pharmacol., 370:157-166, 2004
  3. ^ Birkeland JA. et al., Effects of treatment with a 5-HT4 receptor antagonist in heart failure. Br J Pharmacol. 2007 Jan;150(2):143-52. Epub 2006 Dec 11.