5,253 results match your criteria 5-ht3 receptor


Evaluation of clinical outcomes and efficacy of palonosetron and granisetron in combination with dexamethasone in Egyptian patients receiving highly emetogenic chemotherapy.

Cancer Chemother Pharmacol 2021 Apr 9. Epub 2021 Apr 9.

Medical Oncology Department, Faculty of Medicine, Tanta University, Tanta, Egypt.

Background: Chemotherapy-induced nausea and vomiting (CINV) is considered one of the most serious adverse events affecting chemotherapy-receiving cancer patients. It dramatically affects their food intake, nutritional status and more importantly their quality of life. We can observe CINV in highly emetogenic chemotherapy (HEC) such as adriamycin-cyclophosphamide combination (AC) in breast cancer patients and cisplatin-based regimens in other cancer types. Read More

View Article and Full-Text PDF

Cochlear protection against noise exposure requires serotonin type 3A receptor via the medial olivocochlear system.

FASEB J 2021 May;35(5):e21486

Department of Neuroscience and Cell Biology, Graduate School of Medicine, Osaka University, Suita, Japan.

The cochlear efferent feedback system plays important roles in auditory processing, including regulation of the dynamic range of hearing, and provides protection against acoustic trauma. These functions are performed through medial olivocochlear (MOC) neurons. However, the underlying cellular and molecular mechanisms are not fully understood. Read More

View Article and Full-Text PDF

Treatment with Oral Ondansetron for Ultramarathon-Associated Nausea: The TOO FUN Study.

Sports (Basel) 2021 Mar 3;9(3). Epub 2021 Mar 3.

Physical Medicine and Rehabilitation Service, Department of Veterans Affairs, Northern California Health Care System, Sacramento, CA 95655, USA.

Nausea and vomiting are common for runners during ultramarathons and often contribute to non-finishes. We aimed to determine the efficacy of ondansetron, a commonly used antiemetic, to treat nausea and vomiting in runners during an ultramarathon. Runners who had a previous history of frequent nausea or vomiting during races and entered in 160, 80, and 55 km ultramarathons in 2018 and 2019 were randomized in a double-blind fashion to 4 mg ondansetron or placebo capsules to use if they developed nausea or vomiting during the race with the ability to take three additional doses. Read More

View Article and Full-Text PDF

Does Endogenous Cholecystokinin Modulate Alcohol Intake?

Neuropharmacology 2021 Mar 29:108539. Epub 2021 Mar 29.

Neurobiology of anxiety and mood disorders, University of Nantes, 98, rue Joseph Blanchart, 44100 Nantes, (France). Electronic address:

Alcohol use disorder or alcoholism is characterized by uncontrollable alcohol use and intoxication, as well as a heightened state of anxiety after alcohol withdrawal. Ethanol-associated stimuli also drive the urge to drink by means of classical conditioning. Alcoholism has been considered a dopamine (DA) dysregulation syndrome that involves the activity of the central amygdala circuitry of anxiety. Read More

View Article and Full-Text PDF

Central and peripheral emetic loci contribute to vomiting evoked by the Akt inhibitor MK-2206 in the least shrew model of emesis.

Eur J Pharmacol 2021 Mar 26;900:174065. Epub 2021 Mar 26.

Department of Basic Medical Sciences, College of Osteopathic Medicine of the Pacific, Western University of Health Sciences, 309 East Second Street, Pomona, CA, 91766, USA. Electronic address:

Akt (protein kinase B) signaling is frequently activated in diverse cancers. Akt inhibitors such as perifosine and MK-2206 have been evaluated as potential cancer chemotherapeutics. Although both drugs are generally well tolerated, among their most common side-effects vomiting is a major concern. Read More

View Article and Full-Text PDF

Reciprocal control of obesity and anxiety-depressive disorder via a GABA and serotonin neural circuit.

Mol Psychiatry 2021 Mar 26. Epub 2021 Mar 26.

USDA/ARS Children's Nutrition Research Center, Department of Pediatrics, Baylor College of Medicine, Houston, TX, USA.

The high comorbidity between obesity and mental disorders, such as depression and anxiety, often exacerbates metabolic and neurological symptoms significantly. However, neural mechanisms that underlie reciprocal control of feeding and mental states are largely elusive. Here we report that melanocortin 4 receptor (MC4R) neurons located in the dorsal bed nucleus of the stria terminus (dBNST) engage in the regulation of mentally associated weight gain by receiving GABAergic projections from hypothalamic AgRP neurons onto α5-containing GABA receptors and serotonergic afferents onto 5-HT receptors. Read More

View Article and Full-Text PDF

Serotonin and dopamine receptors profile on peripheral immune cells from patients with temporal lobe epilepsy.

J Neuroimmunol 2021 Mar 5;354:577534. Epub 2021 Mar 5.

Laboratório de Neurofarmacologia, Departamento de Farmacologia, ICB, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, Brazil; Programa de Neurociências, Universidade Federal de Minas Gerais, Belo Horizonte 31270-901, Brazil. Electronic address:

The role of inflammation and immune cells has been demonstrated in neurological diseases, including epilepsy. Leukocytes, as well as inflammatory mediators, contribute to abnormal processes that lead to a reduction in seizure threshold and synaptic reorganization. In this sense, identifying different phenotypes of circulating immune cells is essential to understanding the role of these cells in epilepsy. Read More

View Article and Full-Text PDF

Differential Regulation of Human Serotonin Receptor Type 3A by Chanoclavine and Ergonovine.

Molecules 2021 Feb 24;26(5). Epub 2021 Feb 24.

Department of Biotechnology, Chonnam National University, Gwangju 61186, Korea.

Irritable bowel syndrome (IBS) is a chronic disease that causes abdominal pain and an imbalance of defecation patterns due to gastrointestinal dysfunction. The cause of IBS remains unclear, but intestinal-brain axis problems and neurotransmitters have been suggested as factors. In this study, chanoclavine, which has a ring structure similar to 5-hydroxytryptamine (5-HT), showed an interaction with the 5-HT receptor to regulate IBS. Read More

View Article and Full-Text PDF
February 2021

A phase II study of the safety of olanzapine for oxaliplatin based chemotherapy in coloraectal patients.

Sci Rep 2021 Feb 25;11(1):4547. Epub 2021 Feb 25.

Department of Gastroenterological Surgery, Osaka International Cancer Institute, 3-1-69 Otemae, Chuo-ku, Osaka, Osaka, 541-8567, Japan.

Olanzapine has exhibited efficacy as an antiemetic agent when used with 5-HT receptor antagonists, dexamethasone, and NK receptor antagonists for patients receiving highly emetogenic chemotherapy. In addition, several studies have reported the efficacy or safety of olanzapine in patients receiving moderately emetogenic chemotherapy, including carboplatin, irinotecan, and oxaliplatin. However, no reports of olanzapine use have focused on patients receiving oxaliplatin-based chemotherapy. Read More

View Article and Full-Text PDF
February 2021

Asymmetric opening of the homopentameric 5-HT serotonin receptor in lipid bilayers.

Nat Commun 2021 02 16;12(1):1074. Epub 2021 Feb 16.

Max Planck Institute of Biophysics, Frankfurt am Main, Germany.

Pentameric ligand-gated ion channels (pLGICs) of the Cys-loop receptor family are key players in fast signal transduction throughout the nervous system. They have been shown to be modulated by the lipid environment, however the underlying mechanism is not well understood. We report three structures of the Cys-loop 5-HT serotonin receptor (5HTR) reconstituted into saposin-based lipid bilayer discs: a symmetric and an asymmetric apo state, and an asymmetric agonist-bound state. Read More

View Article and Full-Text PDF
February 2021

Pharmacokinetics and safety evaluation of oral Palonosetron in Chinese healthy volunteers: A phase 1, open-label, randomized, cross-over study.

Eur J Pharm Sci 2021 May 10;160:105752. Epub 2021 Feb 10.

Clinical Pharmacology Research Center, Peking Union Medical College Hospital. Electronic address:

Purpose: Palonosetron hydrochloride is a specific 5-HT3 receptor antagonist, used to prevent chemotherapy-induced nausea and vomiting (CINV), and is a known chemical entity currently registered in the oral and IV forms in several countries worldwide.

Methods: Single-center, single-dose, 3-treatment, open-label, randomized, 3-period, phase-I cross-over study, conducted in 18 individuals (16 males and 2 females). The primary objective was to assess the pharmacokinetic profile of Palonosetron 0. Read More

View Article and Full-Text PDF

The trichothecene neosolaniol stimulates an emetic response through neuropeptide Y2 and serotonin 3 receptors in mink.

Toxicology 2021 Mar 10;452:152718. Epub 2021 Feb 10.

Department of Chemistry, Faculty of Science, University of Hradec Kralove, Hradec Kralove, 50003, Czech Republic. Electronic address:

Type A trichothecene neosolaniol (NEO) is considered a potential risk to human and animal health by the European Food Safety Authority (EFSA). To date, available data do not allow making conclusions about the toxicological properties of this toxin. Trichothecenes have been previously demonstrated to induce emetic responses in mink, and this response has been associated with neurotransmitter peptide YY (PYY) and serotonin (5-hydroxytryptamine, 5-HT). Read More

View Article and Full-Text PDF

Activation of PPG neurons following acute stressors differentially involves hindbrain serotonin in male rats.

Neuropharmacology 2021 04 10;187:108477. Epub 2021 Feb 10.

Department of Psychiatry, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, USA; Department of Biobehavioral Health Sciences, School of Nursing, University of Pennsylvania, Philadelphia, PA, USA. Electronic address:

Within the hindbrain, serotonin (5-HT) functions as a modulator of the central glucagon-like peptide-1 (GLP-1) system. This interaction between 5-HT and GLP-1 is achieved via 5-HT2C and 5-HT3 receptors and is relevant for GLP-1-mediated feeding behavior. The central GLP-1 system is activated by various stressors, activates the hypothalamic pituitary adrenocortical (HPA) axis, and contributes to stress-related behaviors. Read More

View Article and Full-Text PDF

5-HT3/7 and GABA receptors mediate inhibition of trigeminal nociception by dietary supplementation of grape seed extract.

Nutr Neurosci 2021 Feb 5:1-12. Epub 2021 Feb 5.

Missouri State University, Springfield, MO, USA.

Temporomandibular joint disorder is a prevalent orofacial pain condition involving sensitization and activation of trigeminal nociceptive neurons. Dietary supplementation with a proanthocyanin-enriched grape seed extract (GSE) was found to inhibit trigeminal nociception in a chronic TMD model. In this study, the cellular mechanisms by which GSE inhibits sustained trigeminal nociception in male and female Sprague Dawley rats were investigated. Read More

View Article and Full-Text PDF
February 2021

Rostral cuneiform nucleus and the defence reaction: Direct and indirect midbrain-medullary 5-HT mechanisms in baroreflex inhibition.

Br J Pharmacol 2021 Apr;178(8):1819-1835

Sorbonne Université, INSERM, UMRS1158, Neurophysiologie Respiratoire, Expérimentale et Clinique, Paris, France.

Background And Purpose: Activation of the defence reaction inhibits the baroreflex response via the intermediate rostro-ventromedial medulla (B3 raphé) and nucleus tractus solitarius (NTS). Our aim was to determine whether and how baroreflex inhibition, induced by the disinhibition of the rostral cuneiform nucleus (part of the defence pathway), involves 5-HT neurons in B3 and 5-HT receptors in the NTS.

Experimental Approach: We performed immunohistochemistry and anatomical experiments to determine whether raphé 5-HT cells expressing Fos were directly targeted by the rostral cuneiform nucleus. Read More

View Article and Full-Text PDF

A randomized, double-blind, placebo-controlled study to assess efficacy of mirtazapine for the treatment of diarrhea predominant irritable bowel syndrome.

Biopsychosoc Med 2021 Feb 3;15(1). Epub 2021 Feb 3.

Department of Clinical Pharmacy, School of Pharmacy, Hamadan University of Medical Sciences, Shahid Fahmideh Ave, Hamadan, 6517838678, Iran.

Background: Ample evidence indicates the efficacy of serotonin type 3 (5-HT) receptor antagonists in the treatment of patients with diarrhea-predominant irritable bowel syndrome (IBS-D). Mirtazapine is an atypical antidepressant with a well-known 5-HT receptor antagonist property. This study, therefore, was undertaken to investigate whether compared to placebo, mirtazapine would be efficacious and safe in the treatment of patients with IBS-D. Read More

View Article and Full-Text PDF
February 2021

Tropisetron balances immune responses via TLR2, TLR4 and JAK2/STAT3 signalling pathway in LPS-stimulated PBMCs.

Basic Clin Pharmacol Toxicol 2021 May 15;128(5):669-676. Epub 2021 Feb 15.

Reproductive Immunology Research Center, Shahid Sadoughi University of Medical Sciences and Health Services, Yazd, Iran.

Numerous documents have been stated that tropisetron, an antagonist of the 5-HT3 receptor and α7nAChR agonist, modulates immune responses. However, the mechanistic basis for this aspect of tropisetron action is largely unknown. Here, the immuno-modulatory effects of tropisetron are investigated, focusing on the possible molecular targets and the mechanisms. Read More

View Article and Full-Text PDF

Severity of constipation related to palonosetron during first-line chemotherapy: a retrospective observational study.

Support Care Cancer 2021 Jan 29. Epub 2021 Jan 29.

Department of Pharmacy, Saga University Hospital, 5-1-1 Nabeshima, Saga, 849-8501, Japan.

Purpose: Palonosetron, a long-acting 5-HT receptor antagonist, is an effective antiemetic agent for chemotherapy-induced nausea and vomiting; however, it sometimes causes severe constipation. The aim of the present study was to evaluate the severity of palonosetron-related constipation.

Methods: We retrospectively analyzed the incidence and severity of constipation after intravenous administration of 0. Read More

View Article and Full-Text PDF
January 2021

Serotonin Plays a Key Role in the Development of Opioid-Induced Hyperalgesia in Mice.

J Pain 2021 Jan 16. Epub 2021 Jan 16.

Division of Anesthesiology, Niigata University Graduate School of Medical and Dental Sciences, Niigata City, Japan.

Opioid usage for pain therapy is limited by its undesirable clinical effects, including paradoxical hyperalgesia, also known as opioid-induced hyperalgesia (OIH). However, the mechanisms associated with the development and maintenance of OIH remain unclear. Here, we investigated the effect of serotonin inhibition by the 5-HT receptor antagonist, ondansetron (OND), as well as serotonin deprivation via its synthesis inhibitor para-chlorophenylalanine, on mouse OIH models, with particular focus on astrocyte activation. Read More

View Article and Full-Text PDF
January 2021

Role of peripheral 5-HT, 5-HT and 5-HT receptors in the mechanical allodynia induced by serotonin in mice.

Biomed Pharmacother 2021 Mar 1;135:111210. Epub 2021 Feb 1.

Department of Pharmaceutical Products, School of Pharmacy, Federal University of Minas Gerais, Avenida Antônio Carlos 6627, 31270-901, Belo Horizonte, Brazil.

Serotonin (5-HT) acts as a neurotransmitter in the central nervous system (CNS) and as a mediator released by enterochromaffin cells to regulate intestinal motility. However, this amine also plays an important role as an inflammatory mediator and induces phenotypic changes of nociceptors. Despite the wide knowledge of the role of 5-HT in nociception, most studies have focused on its role in the CNS, while a clear information about its role in peripheral tissues is still lacking. Read More

View Article and Full-Text PDF

Prophylactic antiemetic effects of dexamethasone versus 5-HT3 receptor antagonists in ear surgery: a systematic review and meta-analysis.

Int J Clin Pharm 2021 Jan 13. Epub 2021 Jan 13.

Department of Anesthesiology, Chung Shan Medical University Hospital and Institute of Medicine, Chung Shan Medical University, Taichung, Taiwan.

Background The optimal strategy for reducing the high incidence of postoperative nausea and vomiting (PONV) after otologic surgical procedures remains inconclusive. Aim of the review This study compared the prophylactic antiemetic effects of dexamethasone with 5-hydroxytryptamine 3 receptor antagonists (5-HT3-RAs) in ear surgery. Method PubMed, Embase, and Cochrane Library were searched up to October 31, 2020 for randomized controlled trials that used dexamethasone either singly or in combination with 5-HT3-RAs for PONV prophylaxis in adults undergoing ear surgery. Read More

View Article and Full-Text PDF
January 2021

NMDA receptor-independent LTP in mammalian nervous system.

Authors:
Karim A Alkadhi

Prog Neurobiol 2021 May 2;200:101986. Epub 2021 Jan 2.

Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX, 77204, USA. Electronic address:

Long-term potentiation (LTP) of synaptic transmission is a form of activity-dependent synaptic plasticity that exists at most synapses in the nervous system. In the central nervous system (CNS), LTP has been recorded at numerous synapses and is a prime candidate mechanism associating activity-dependent plasticity with learning and memory. LTP involves long-lasting increase in synaptic strength with various underlying mechanisms. Read More

View Article and Full-Text PDF

Granisetron, a selective 5-HT3 antagonist, reduces L-3,4-dihydroxyphenylalanine-induced abnormal involuntary movements in the 6-hydroxydopamine-lesioned rat.

Behav Pharmacol 2021 Feb;32(1):43-53

Neurodegenerative Disease Group, Montreal Neurological Institute.

Administration of L-3,4-dihydroxyphenylalanine (L-DOPA) provides Parkinson's disease patients with effective symptomatic relief. However, long-term L-DOPA therapy is often marred by complications such as dyskinesia. We have previously demonstrated that serotonin type 3 (5-HT3) receptor blockade with the clinically available and highly selective antagonist ondansetron alleviates dyskinesia in the 6-hydroxydopamine (6-OHDA)-lesioned rat. Read More

View Article and Full-Text PDF
February 2021

Fixed-Dose Netupitant and Palonosetron for Chronic Nausea in Cancer Patients: A Double-Blind, Placebo Run-in Pilot Randomized Clinical Trial.

J Pain Symptom Manage 2021 Jan 1. Epub 2021 Jan 1.

Department of Palliative Care, Rehabilitation and Integrative Medicine, MD Anderson Cancer Center, Houston, Texas, USA.

Context: No clinical trials have examined the effect of netupitant/palonosetron (NEPA) on chronic nausea in patients with cancer.

Objectives: In this pilot randomized trial, we assessed the efficacy of NEPA and placebo on chronic nausea.

Methods: This double-blind, parallel, randomized trial enrolled patients with cancer and chronic nausea for at least 1 month, intensity ≥4/10 and not on moderately or highly emetogenic systemic therapies. Read More

View Article and Full-Text PDF
January 2021

Chemotherapy-Induced Nausea and Vomiting: Pathogenesis, Recommendations, and New Trends.

Cancer Treat Res Commun 2021 11;26:100278. Epub 2020 Dec 11.

Vardhaman Mahavir Medical College and Safdurjung Hospital, New Delhi 110029, India.

The significant physical and emotional effects of chemotherapy-induced nausea and vomiting (CINV) are experienced by cancer patients. Severe symptoms decrease the patient's quality of life and potentially deters further treatment. The five main forms of CINV (i. Read More

View Article and Full-Text PDF
December 2020

Mitochondrial Membranes of Human SH-SY5Y Neuroblastoma Cells Express Serotonin 5-HT Receptor.

Int J Mol Sci 2020 Dec 17;21(24). Epub 2020 Dec 17.

Biofordrug srl, via Dante 99, 70019 Triggiano (Bari), Italy.

Mitochondria in neurons contribute to energy supply, the regulation of synaptic transmission, Ca homeostasis, neuronal excitability, and stress adaptation. In recent years, several studies have highlighted that the neurotransmitter serotonin (5-HT) plays an important role in mitochondrial biogenesis in cortical neurons, and regulates mitochondrial activity and cellular function in cardiomyocytes. 5-HT exerts its diverse actions by binding to cell surface receptors that are classified into seven distinct families (5-HT1 to 5-HT7). Read More

View Article and Full-Text PDF
December 2020

What is the ideal combination antiemetic regimen?

Best Pract Res Clin Anaesthesiol 2020 Dec 4;34(4):701-712. Epub 2020 Nov 4.

Department of Anesthesiology, Stony Brook University, Stony Brook, NY, USA.

Postoperative nausea and vomiting (PONV) and post-discharge nausea and vomiting (PDNV) are frequent unpleasant complaints that patients and clinicians report after surgery. PONV and PDNV have been associated with postoperative complications and hospital discharge delays. Despite the extensive evidence describing the use of several regimens in different surgical populations, the ideal regimen has not been established. Read More

View Article and Full-Text PDF
December 2020

Ethanol induces persistent potentiation of 5-HT receptor-stimulated GABA release at synapses on rat hippocampal CA1 neurons.

Neuropharmacology 2021 02 1;184:108415. Epub 2020 Dec 1.

Section on Synaptic Pharmacology, Laboratory for Integrative Neuroscience, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, MD, 20892, USA. Electronic address:

Several studies have shown that ethanol (EtOH) can enhance the activity of GABAergic synapses via presynaptic mechanisms, including in hippocampal CA1 neurons. The serotonin type 3 receptor (5-HT-R) has been implicated in the neural actions of ethanol (EtOH) and in modulation of GABA release from presynaptic terminals. In the present study, we investigated EtOH modulation of GABA release induced by 5-HT-R activation using the mechanically isolated neuron/bouton preparation from the rat CA1 hippocampal subregion. Read More

View Article and Full-Text PDF
February 2021

5HT RA plus dexamethasone plus aprepitant for controlling delayed chemotherapy-induced nausea and vomiting in colorectal cancer.

Cancer Sci 2021 Feb 17;112(2):744-750. Epub 2020 Dec 17.

Department of Pharmaceutical and Health Care Management, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan.

Delayed chemotherapy-induced nausea and vomiting (CINV) is not well controlled in colorectal cancer (CRC) patients undergoing oxaliplatin (L-OHP)-based chemotherapy. Whether neurokinin-1 receptor antagonist addition to a first-generation 5HT antagonist (1st 5-HT RA) and dexamethasone (DEX) is beneficial to these patients remains controversial. Furthermore, whether palonosetron (PALO) or aprepitant (APR) is more effective in controlling delayed CINV is unclear. Read More

View Article and Full-Text PDF
February 2021