Piboserod is a selective 5-HT₄ receptor antagonist which was marketed and manufactured by

GlaxoSmithKline GSK plc, formerly GlaxoSmithKline plc, is a British Multinational corporation, multinational pharmaceutical and biotechnology company with global headquarters in London, England. Established in 2000 by a Mergers and acquisitions, merger of Gl ...

(GSK) under the trade name Serlipet for the management of atrial fibrillation and

irritable bowel syndrome Irritable bowel syndrome (IBS) is a "disorder of gut-brain interaction" characterized by a group of symptoms that commonly include abdominal pain and or abdominal bloating and changes in the consistency of bowel movements. These symptoms ma ...

. In 2007 the Norwegian company Bio-Medisinsk Innovasjon AS (BMI) completed a clinical phase II study to investigate the effect of piboserod in patients with chronic

heart failure Heart failure (HF), also known as congestive heart failure (CHF), is a syndrome, a group of signs and symptoms caused by an impairment of the heart's blood pumping function. Symptoms typically include shortness of breath, excessive fatigue, ...

Mechanism of action

In 2002 a research group at the

University of Oslo The University of Oslo ( no, Universitetet i Oslo; la, Universitas Osloensis) is a public research university located in Oslo, Norway. It is the highest ranked and oldest university in Norway. It is consistently ranked among the top univers ...

discovered that muscles from the ventricle of failing hearts have increased responsiveness to serotonin. They later demonstrated that the effect was due to an

expression Expression may refer to: Linguistics * Expression (linguistics), a word, phrase, or sentence * Fixed expression, a form of words with a specific meaning * Idiom, a type of fixed expression * Metaphorical expression, a particular word, phrase, ...

of functional 5-HT₄ receptors in the failing muscle. On the basis of these findings, and in analogy with the success of

betablocker Beta blockers, also spelled β-blockers, are a class of medications that are predominantly used to manage abnormal heart rhythms, and to protect the heart from a second heart attack after a first heart attack (secondary prevention). They are al ...

s 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 model An animal model (short for animal disease model) is a living, non-human, often genetic-engineered animal used during the research and investigation of human disease, for the purpose of better understanding the disease process without the risk of ha ...

s of heart failure with positive results.

References

{{GlaxoSmithKline 5-HT4 antagonists Piperidines Carboxamides Indoles GSK plc brands