Piboserod
Encyclopedia
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) completed a clinical phase II study to investigate the effect of piboserod in patients with chronic heart failure.
. 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 model
s of heart failure with positive results.
5-HT4 receptor
5-hydroxytryptamine receptor 4 is a protein that in humans is encoded by the HTR4 gene.- Location :The receptor is located in the alimentary tract, urinary bladder, heart and adrenal gland as well as the central nervous system ....
receptor antagonist
Antagonist
An antagonist is a character, group of characters, or institution, that represents the opposition against which the protagonist must contend...
which was marketed and manufactured by GlaxoSmithKline
GlaxoSmithKline
GlaxoSmithKline plc is a global pharmaceutical, biologics, vaccines and consumer healthcare company headquartered in London, United Kingdom...
(GSK) under the trade name Serlipet for the management of atrial fibrillation
Atrial fibrillation
Atrial fibrillation is the most common cardiac arrhythmia . It is a common cause of irregular heart beat, identified clinically by taking a pulse. Chaotic electrical activity in the two upper chambers of the heart result in the muscle fibrillating , instead of achieving coordinated contraction...
and irritable bowel syndrome
Irritable bowel syndrome
Irritable bowel syndrome is a diagnosis of exclusion. It is a functional bowel disorder characterized by chronic abdominal pain, discomfort, bloating, and alteration of bowel habits in the absence of any detectable organic cause. In some cases, the symptoms are relieved by bowel movements...
. 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.
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 serotoninSerotonin
Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...
. 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 model
Animal model
An animal model is a living, non-human animal used during the research and investigation of human disease, for the purpose of better understanding the disease without the added risk of causing harm to an actual human being during the process...
s of heart failure with positive results.