5-HT4 Receptors contribute to the motor stimulating effect of levosulpiride in the guinea-pig gastrointestinal tract

Tonini, Marcello; Giorgio, Roberto De; Spelta, Valeria; Bassotti, Gabrio; Nucci, A. Di; Anselmi, Laura; Balestra, B.; Ponti, Fabrizio De

doi:10.1016/s1590-8658(03)00061-6

Cited by 19 publications

(23 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Many prokinetic agents available on the market are, in fact, antagonists of D 2 receptor. Surprisingly, some of these antagonists, such as levosulpiride and metoclopramide, also share partial to moderate agonistic activity on 5-HT4R (Tonini, 1996;Tonini et al, 2003). Therefore, it is plausible that PF-W may interact with the enteric dopaminergic system, which should be explored through further experiments.…”

Section: Discussionmentioning

confidence: 99%

An aqueous extract of Poncirus fructus activates the prokinetic activity of 5-HT receptor subtype 4 without hERG interaction

Shim¹,

Back²,

Jung³

et al. 2010

Journal of Ethnopharmacology

View full text Add to dashboard Cite

Section: Discussionmentioning

confidence: 99%

An aqueous extract of Poncirus fructus activates the prokinetic activity of 5-HT receptor subtype 4 without hERG interaction

Shim¹,

Back²,

Jung³

et al. 2010

Journal of Ethnopharmacology

View full text Add to dashboard Cite

“…Levosulpiride is a benzamide derivative, which selectively inhibits D 2 receptors and also interacts with 5-HT 4 receptors, and to a lesser extent with 5-HT 3 receptors [24,25] . It has been suggested that the serotonergic component possessed by levosulpiride may enhance its therapeutic effi cacy in stimulating gastric and small bowel motility [25] .…”

Section: Levosulpiridementioning

confidence: 99%

“…It has been suggested that the serotonergic component possessed by levosulpiride may enhance its therapeutic effi cacy in stimulating gastric and small bowel motility [25] .…”

Section: Levosulpiridementioning

confidence: 99%

Promotility Medications – Now and in the Future

Karamanolis

Tack²

2006

Dig Dis

View full text Add to dashboard Cite

Gastrointestinal promotility drugs stimulate smooth muscle contractions to enhance gastric emptying and small and large bowel transit. Currently available drug classes with prokinetic properties include antidopaminergic agents, serotonergic agents, and motilin-receptor agonists. Due to moderate prokinetic effects, poor symptomatic responses and the presence of adverse effects, there is a clear need for new classes of prokinetics. Several newer prokinetic drugs and drug classes are currently under evaluation. Selecting candidate agents and designing the appropriate therapeutic trials is hampered by the lack of insight in the pathophysiology of motility-related symptoms. As gastrointestinal motor disorders are chronic, relapsing, and remitting disorders, it seems desirable that studies with candidate prokinetic drugs establish a long-term efficacy and not only short-term effects on gastrointestinal functions.

show abstract

“…Hyperprolactinemia is an additional side effect. Levosulpiride has a pharmacological profi le similar to that of metoclopramide (but with a lower 5-HT 3 affi nity) [72] . It has been shown to improve symptoms in functional dyspepsia [73,74] , and to reduce gastric sensation to distension [75] .…”

Section: -Htmentioning

confidence: 99%

Drugs Acting on Serotonin Receptors for the Treatment of Functional GI Disorders

Tonini

Pace

2006

Dig Dis

View full text Add to dashboard Cite

In the gut, serotonin (5-hydroxytryptamine: 5-HT) exerts a variety of effects on intrinsic enteric neurons, extrinsic afferents, enterocytes and smooth muscle cells, which are related to the expression of multiple 5-HT receptor types and subtypes regulating motility, vascular tone, secretion and perception. Agonists and antagonists at 5-HT receptors have gained access to the market for the two major variants of the irritable bowel syndrome (IBS), a functional disorder characterized by abdominal pain associated with diarrhea and/or constipation in the absence of any organic abnormality. Indeed, the 5-HT₃ receptor antagonist alosetron is available in the US market for the treatment of women with severe, diarrhea-predominant IBS (D-IBS) refractory to conventional therapy, whereas tegaserod, a partial 5-HT₄ receptor agonist, has been approved by the FDA and other regulatory agencies for the treatment of women with constipation-predominant IBS (C-IBS) or functional constipation. This review is mainly intended to discuss the role of non-neuronal (paracrine) and neuronal 5-HT in the pathophysiology of functional gastrointestinal disorders (FGIDs), such as IBS and functional dyspepsia, and the mechanisms through which drugs acting on 5-HT receptors regulate visceral motility, perception and secretion in these two conditions.

show abstract

5-HT4 Receptors contribute to the motor stimulating effect of levosulpiride in the guinea-pig gastrointestinal tract

Cited by 19 publications

References 28 publications

An aqueous extract of Poncirus fructus activates the prokinetic activity of 5-HT receptor subtype 4 without hERG interaction

An aqueous extract of Poncirus fructus activates the prokinetic activity of 5-HT receptor subtype 4 without hERG interaction

Promotility Medications – Now and in the Future

Drugs Acting on Serotonin Receptors for the Treatment of Functional GI Disorders

Contact Info

Product

Resources

About