The facilitating effect of prucalopride on cholinergic neurotransmission in pig gastric circular muscle is regulated by phosphodiesterase 4

Priem, Evelien; Colen, Inge Van; Maeyer, Joris H. De; Lefebvre, Romain

doi:10.1016/j.neuropharm.2011.12.020

Cited by 21 publications

(30 citation statements)

References 35 publications

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“…5HT-3R antagonists are used to treat diarrhoea-type IBS and 5HT-4R agonists have been proved in the treatment of constipation-type IBS and chronic constipation 5–7. Prucalopride, a highly selective 5HT-4R agonist, has received special attention as it is a potent stimulator of gut motility8 9 and exerts facilitating actions on gut smooth muscle cells 10. This effect could be proved in large randomised trials in which prucalopride was effective in the treatment of chronic constipation 11.…”

Section: Introductionmentioning

confidence: 99%

The enteric serotonergic system is altered in patients with diverticular disease

Böttner

Barrenschee

Hellwig

et al. 2012

Gut

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Section: Introductionmentioning

confidence: 99%

The enteric serotonergic system is altered in patients with diverticular disease

Böttner

Barrenschee

Hellwig

et al. 2012

Gut

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“…Following this initial report, numerous selective 5-HT4 receptor agonists have been recognized that target 5-HT4 receptors in the central nervous system and peripheral organs and tissues262728, and which thus have great therapeutic potential to treat patients suffering from a variety of diseases. In different peripheral organs, including the gastro intestinal (GI) tract, heart, and lung, 5-HT4 receptor activation is involved in various physiological processes293031. For example, 5-HT4 receptor activation mediates peristaltic reflex activity due to its impaction on the enteric cholinergic axis32 and reversion of respiratory depression in etorphine-immobilisation33.…”

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confidence: 99%

Identification and functional characterisation of 5-HT4 receptor in sea cucumber Apostichopus japonicus (Selenka)

Wang

Yang

Zhou

et al. 2017

Sci Rep

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Serotonin (5-HT) is an important neurotransmitter and neuromodulator that controls a variety of sensory and motor functions through 5-HT receptors (5-HTRs). The 5-HT4R subfamily is linked to Gs proteins, which activate adenylyl cyclases (ACs), and is involved in many responses in peripheral organs. In this study, the 5-HT4R from Apostichopus japonicus (Aj5-HT4R) was identified and characterised. The cloned full-length Aj5-HT4R cDNA is 1,544 bp long and contains an open reading frame 1,011 bp in length encoding 336 amino acid proteins. Bioinformatics analysis of the Aj5-HT4R protein indicated this receptor was a member of class A G protein coupled receptor (GPCR) family. Further experiments using Aj5-HT4R-transfected HEK293 cells demonstrated that treatment with 5-HT triggered a significant increase in intracellular cAMP level in a dose-dependent manner and induced a rapid internalisation of Aj5-HT4R fused with enhanced green fluorescent protein (Aj5-HT4R-EGFP) from the cell surface into the cytoplasm. In addition, the transcriptional profiles of Aj5-HT4R in aestivating A. japonicas and phosphofructokinase (AjPFK) in 5-HT administrated A. japonicus have been analysed by real-time PCR assays. Results have led to a basic understanding of Aj5-HT4R in A. japonicus, and provide a foundation for further exploration of the cell signaling and regulatory functions of this receptor.

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“…Prior experiments in animals indicated that prucalopride also effects contractility of the stomach [20,21] Moreover, a positive effect on gastric motility was already observed in the chronic constipated patient. In our patients, prucalopride led to an accelerated overall gastric emptying and small bowel transit which we believe to be the main effect of prucalopride on GERD [22].…”

Section: Discussionmentioning

confidence: 99%

Prucalopride reduces the number of reflux episodes and improves subjective symptoms in gastroesophageal reflux disease: a case series

et al. 2014

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IntroductionTreatment of persistence to proton pump inhibitors or non-acid reflux episodes in patients with gastroesophageal reflux disease is challenging. Prucalopride, a selective high affinity serotonin (5-HT4) receptor agonist, might offer a possible new therapeutic alterative.Case presentationsWe report four chronically constipated female gastroesophageal reflux disease-patients with reflux symptoms and an increased number of reflux episodes in combined esophageal pH and multichannel impedance monitoring treated with prucalopride (2mg per day). Symptoms were persistent to proton pump inhibitors and ranitidine. Gastroesophageal reflux was detected by pH or multichannel impedance (MII) monitoring. Numbers of all reflux episodes as well as non-acid reflux episodes were reduced in all of our patients. The objective findings were concordant with subjective reports of symptom relief. There were no major adverse events in any patient during therapy with prucalopride.ConclusionAdministration of prucalopride showed promising results in the treatment of persisting or weakly and/or non-acid reflux episodes in our case series in four constipated patients. Therefore, prucalopride can be regarded as a possible therapeutic option in the treatment of standard proton pump inhibitor-persistent reflux in the chronically constipated patient. However, further prospective trials are needed to prove our findings.

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The facilitating effect of prucalopride on cholinergic neurotransmission in pig gastric circular muscle is regulated by phosphodiesterase 4

Cited by 21 publications

References 35 publications

The enteric serotonergic system is altered in patients with diverticular disease

The enteric serotonergic system is altered in patients with diverticular disease

Identification and functional characterisation of 5-HT4 receptor in sea cucumber Apostichopus japonicus (Selenka)

Prucalopride reduces the number of reflux episodes and improves subjective symptoms in gastroesophageal reflux disease: a case series

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