5-HT4 Serotonin Receptors

A subtype of G-protein-coupled SEROTONIN receptors that preferentially couple to GS STIMULATORY G-PROTEINS resulting in increased intracellular CYCLIC AMP. Several isoforms of the receptor exist due to ALTERNATIVE SPLICING of its mRNA.

Also Known As:

Receptors, Serotonin, 5-HT4; 5-HT4 Receptor; 5-HT4L Receptor; 5-HT4S Receptor; 5-Hydroxytryptamine-4 Receptor; Receptor, Serotonin 4; Serotonin 4 Receptors; 5 HT4 Receptor; 5 HT4L Receptor; 5 HT4S Receptor; 5 Hydroxytryptamine 4 Receptor; Receptor, 5-HT4; Receptor, 5-HT4L; Receptor, 5-HT4S; Receptor, 5-Hydroxytryptamine-4; Receptors, Serotonin 4; Receptors, Serotonin, 5-HT4L; Receptors, Serotonin, 5-HT4S; Serotonin 4 Receptor

Networked: 197 relevant articles (15 outcomes, 26 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Amino Acids, Peptides, and Proteins: 1
- Proteins: 484843
  - Membrane Proteins: 10078
    - Cell Surface Receptors: 2125

Experts

1.	Lefebvre, Hervé: 5 articles (06/2020 - 01/2003)
2.	Bockaert, Joël: 5 articles (11/2017 - 01/2004)
3.	Tack, Jan: 4 articles (01/2021 - 08/2009)
4.	Louiset, Estelle: 4 articles (06/2020 - 05/2005)
5.	Nasehi, Mohammad: 4 articles (01/2020 - 03/2014)
6.	Lezoualc'h, Frank: 4 articles (04/2009 - 04/2007)
7.	Cartier, Dorthe: 4 articles (12/2005 - 03/2002)
8.	Kuhn, Jean-Marc: 4 articles (12/2005 - 03/2002)
9.	Vaudry, Hubert: 4 articles (12/2005 - 03/2002)
10.	Duparc, Céline: 3 articles (06/2020 - 05/2005)

Related Diseases

1.	Constipation 01/01/2022 - "5-HT4 receptor antagonists are recommended in refractory constipation. " 10/01/2019 - "The prokinetic effects of 5-HT4 receptor (5-HT4 R) agonists have been utilized clinically for almost three decades to relieve symptoms of constipation. " 10/01/2019 - "The model recapitulates healthy and slow transit constipation phenotypes, and the effect of a 5-HT4 receptor agonist in healthy volunteers. " 12/01/2014 - "Adverse effects of previously developed 5-HT4 receptor agonists to treat functional constipation (FC) and constipation IBS (IBS-C) patients have limited their use but have given rise to new and more selective 5-HT4 receptor agonists. " 01/01/2001 - "A related class of drugs, the 5-HT4 receptor agonists, is being developed for the treatment of constipation-predominant IBS. "
2.	Irritable Bowel Syndrome (Syndrome, Irritable Bowel) 10/31/2017 - "miR-16 and miR-103 impact 5-HT4 receptor signalling and correlate with symptom profile in irritable bowel syndrome." 11/01/1999 - "To investigate the effects of SB-207266-A, a selective 5-HT4 receptor antagonist on rectal sensitivity and small bowel transit in patients with irritable bowel syndrome. " 11/01/1999 - "5-HT4 receptor antagonism in irritable bowel syndrome: effect of SB-207266-A on rectal sensitivity and small bowel transit." 04/01/2005 - "To evaluate the safety/tolerability and efficacy of tegaserod, a 5-HT4 receptor partial agonist, in the treatment of patients with non-diarrhoea irritable bowel syndrome (non-D-IBS) in Switzerland. " 03/01/1999 - "Novartis is developing Zelmac (SDZ-HTF-919), a 5-HT4 receptor partial agonist, which is in phase III clinical trials for the treatment of gastric motility disorders and irritable bowel syndrome (IBS). "
3.	Gastroparesis 01/01/2021 - "Randomised study: effects of the 5-HT4 receptor agonist felcisetrag vs placebo on gut transit in patients with gastroparesis." 04/01/2016 - "Randomized clinical trial: a controlled pilot trial of the 5-HT4 receptor agonist revexepride in patients with symptoms suggestive of gastroparesis." 01/01/2006 - "Mosapride citrate, a 5-HT4 receptor agonist, enhances gastric emptying and alleviates gastrointestinal discomfort in patients with diabetic gastroparesis. " 03/30/2021 - "The 5-HT4 receptor is an attractive therapeutic target since it has a potential role in central and peripheral nervous system disorders such as AD, irritable bowel syndrome, and gastroparesis. " 10/01/1996 - "These advances have led to the development of several selective 5-HT4 receptor agonists and antagonists that may have therapeutic utility in the treatment of peripheral disorders such as irritable bowel syndrome, gastroparesis, urinary incontinence and cardiac arrhythmias."
4.	Major Depressive Disorder (Major Depressive Disorders) 01/01/2023 - "Serotonin 4 Receptor Brain Binding in Major Depressive Disorder and Association With Memory Dysfunction." 01/01/2023 - "The cerebral serotonin 4 (5-HT4) receptor is a promising novel target for treatment of major depressive disorder (MDD), and pharmacological stimulation of the 5-HT4 receptor has been associated with improved learning and memory in healthy individuals. " 01/01/2023 - "Stress Hormone Dynamics Are Coupled to Brain Serotonin 4 Receptor Availability in Unmedicated Patients With Major Depressive Disorder: A NeuroPharm Study." 01/01/2020 - "Predicting Treatment Outcome in Major Depressive Disorder Using Serotonin 4 Receptor PET Brain Imaging, Functional MRI, Cognitive-, EEG-Based, and Peripheral Biomarkers: A NeuroPharm Open Label Clinical Trial Protocol."
5.	Hypersensitivity (Allergy) 05/05/2018 - "DSP-6952, a novel 5-HT4 receptor partial agonist, inhibits visceral hypersensitivity and ameliorates gastrointestinal dysfunction in experimental animals." 12/01/1996 - "5-HT4 receptor antagonists, by contrast, reduce 5-HT-induced enteric nerve hypersensitivity without notably affecting the function of the normal bowel. " 05/05/2018 - "It was concluded that DSP-6952, a novel and orally available 5-HT4 receptor agonist, induced colonic GMCs, enhanced colonic transit, increased defecation without inducing diarrhea, improved drug-induced delay in whole-gut transit, and inhibited visceral hypersensitivity in experimental animals. " 01/14/2004 - "Attenuated response to stress and novelty and hypersensitivity to seizures in 5-HT4 receptor knock-out mice." 12/01/2014 - "This work was aimed to evaluate the influence of YKP10811, a new potent 5-HT4 receptor partial agonist, on rat models of colorectal hypersensitivity to distension. "

Related Drugs and Biologics

1.	tegaserod (Zelnorm)
2.	Serotonin (5 Hydroxytryptamine)
3.	prucalopride
4.	zacopride
5.	5-HT3 Serotonin Receptors (5 HT3 Receptor)
6.	mosapride
7.	Acids
8.	5-HT2A Serotonin Receptor (5 HT2A Receptor)
9.	Ketanserin
10.	Esters

Related Therapies and Procedures

1.	Therapeutics
2.	Electroacupuncture
3.	Drug Therapy (Chemotherapy)
4.	Nutritional Support (Artificial Feeding)
5.	Analgesia