Desensitization of 5-HT(4) receptors is regulated by G-protein coupled receptor kinases (GRKs). However, the specific GRK(s) that regulates the desensitization of 5-HT(4) receptors in the in vivo setting is unknown. We investigated the in situ expression of 5-HT(4) receptors and the GRKs in the rat gastrointestinal tract using immunohistochemistry and their interaction using coimmunoprecipitation. 5-HT(4) receptors were expressed in the tunica muscularis mucosae of the oesophagus, longitudinal muscle, myenteric plexus, circular muscle, submucosal plexus and muscularis mucosae of both the proximal and distal colon. GRK2 was expressed in longitudinal muscle and occasionally in myenteric plexus whilst GRK5 showed limited expression in the nerve endings of the myenteric plexus and submucosal plexus of the colon. GRK3 was expressed in the tunica muscularis mucosae of the oesophagus, circular muscle, submucosal plexus and muscularis mucosae of the colon. GRK6 was expressed in the tunica muscularis mucosae of the oesophagus, longitudinal muscle, circular muscle, and muscularis mucosae of the colon. Stimulation of tunica muscularis mucosae of the oesophagus and distal colon using the 5-HT(4) receptor agonist, tegaserod, followed by analysis of the 5-HT(4) receptor antibody immunoprecipitate, revealed the coimmunoprecipitation of GRK6 with 5-HT(4) receptors in the tunica muscularis mucosae of oesophagus while GRK2 and GRK6 were coimmunoprecipitated with 5-HT(4) receptors in the distal colon. This study indicates that GRK6 may be involved in the regulation of the desensitization of 5-HT(4) receptors in the rat oesophagus whilst GRK2 and GRK6 may be involved in regulation of the desensitization of 5-HT(4) receptors in the distal colon.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bcp.2010.09.003 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Investigating the Mechanisms Involved in Scopolamine-induced Memory Degradation.
Arch Razi Inst
June 2024
Medical Plants Research Center, Basic Health Sciences Institute, Shahrekord University of Medical Sciences, Shahrekord, Iran.
In the present study, the mechanisms involved in scopolamine-induced memory impairment have been investigated. The molecular events that take place during memory mostly include mechanisms that are seen in the acquisition phase. Results showed that one of the mechanisms of memory destruction caused by scopolamine, in addition to weakening the cholinergic system, is the indirect effect of scopolamine on other neurotransmitter systems, including the glutamatergic system.
View Article and Find Full Text PDFTargeting serotonin receptors with phytochemicals - an in-silico study.
Sci Rep
December 2024
Department of Management, Bar-Ilan University, Ramat Gan, 5290002, Israel.
Article Synopsis
- * An evaluation of 88 phytochemicals identified five (Genistein, Kaempferol, Daidzein, Peonidin, and glycitein) with strong pharmacokinetic properties and effective binding to serotonin receptors.
- * The study suggests these phytochemicals, commonly found in soybeans and various plants, could lead to natural depression treatments, but more research is needed to confirm their effectiveness in real-world applications.
Zuojin Pill enhances gastrointestinal motility by modulating the pacemaker potentials in interstitial cells of Cajal through multiple signaling pathways.
Int J Med Sci
December 2024
Department of Longevity and Biofunctional Medicine, School of Korean Medicine, Pusan National University, Yangsan 50612, Republic of Korea.
Article Synopsis
- Zuojin Pill (ZJP) is a traditional herbal remedy aimed at treating gastrointestinal disorders, and the study explores how it affects interstitial cells of Cajal (ICCs) and gut movement in mice.
- The research found that ZJP depolarizes ICCs, reducing their pacemaker activity and affecting calcium signaling, which is crucial for normal GI motility; this process is influenced by specific receptor interactions and various signaling pathways.
- Additionally, ZJP improved intestinal transit in mouse models of GI motility disorders and increased levels of key substances that promote gut movement, suggesting its potential as a therapeutic agent in digestive health.
Changes in hippocampal volume, 5-HT receptor binding, and verbal memory over the course of antidepressant treatment in major depressive disorder.
J Psychiatr Res
November 2024
Neurobiology Research Unit and BrainDrugs, Copenhagen University Hospital Rigshospitalet, Copenhagen, Denmark; Mental Health Center Copenhagen, Copenhagen University Hospital - Mental Health Services CPH, Copenhagen, Denmark; Department of Clinical Medicine, University of Copenhagen, Copenhagen, Denmark.
Article Synopsis
- - Serotonin reuptake inhibitors may help boost memory and increase hippocampal volume in patients with Major Depressive Disorder (MDD), particularly through the involvement of the 5-HT4 receptor. - In a study with 91 patients, significant reductions in hippocampal volume were observed after 8 weeks of treatment, especially in those responding well to the antidepressant escitalopram. - The research indicated a negative relationship between 5-HT4 receptor binding and hippocampal volume in females, suggesting a complex interaction that needs further exploration to understand its impact on memory and brain plasticity in MDD.
Electroacupuncture versus 5-HT4 receptor agonist for functional constipation: A systematic review and meta-analysis of randomized controlled trials.
Medicine (Baltimore)
November 2024
Department of Oncology, The Affiliated Taizhou People's Hospital of Nanjing Medical University, Taizhou, China.
Background: Functional constipation (FC) has been found as a chronic gastrointestinal disease that is commonly diagnosed in patients. However, patients have a low satisfaction level with the treatment of constipation drugs (e.g.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!