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5 ht3

Awanish Mishra, Rajesh Kumar Goel
Our previous studies have suggested a strong involvement of serotonergic innervations in epileptogenesis and associated memory impairment. Several studies have suggested that the modulation of 5-HT3 receptors could serve as a promising tool for the management of epilepsy and memory deficit. The present study was envisaged to confirm this hypothesis. In this study, kindling was induced in male Swiss Albino mice by using a subconvulsive dose of pentylenetetrazole (PTZ) (35 mg/kg at 48±2 h). Once the animals were kindled, they were treated with a vehicle, ondansetron (0...
October 13, 2016: Neuroscience
Carl L Faingold, Marcus Randall, Chang Zeng, Shifang Peng, Xiaoyan Long, Hua-Jun Feng
Drugs that enhance the action of serotonin (5-hydroxytrypamine, 5-HT), including several selective serotonin reuptake inhibitors (SSRIs), reduce susceptibility to seizure-induced respiratory arrest (S-IRA) that leads to death in the DBA/1 mouse model of sudden unexpected death in epilepsy (SUDEP). However, it is not clear if specific 5-HT receptors are important in the action of these drugs and whether the brain is the major site of action of these agents in this SUDEP model. The current study examined the actions of agents that affect the 5-HT3 receptor subtype on S-IRA and whether intracerebroventricular (ICV) microinjection of an SSRI would reduce S-IRA susceptibility in DBA/1 mice...
October 12, 2016: Epilepsy & Behavior: E&B
Jonathan H Rapp, Meggie Yuen, Teena Abraham
PURPOSE: There have been 3 published reports (4 cases) of symptomatic sinus bradycardia occurring after intravenous (IV) administration of the selective 5-hydroxytryptamine 3 (5-HT3) receptor antagonist ondansetron. We report a fifth case in which the patient developed asystole after rechallenge with ondansetron. SUMMARY: A 36-year-old pregnant patient with no cardiac history, status post cerclage for cervical insufficiency, experienced nausea in the post ambulatory care unit after administration of morphine and indomethacin for pain...
November 2015: Hospital Pharmacy
Fang Li, Jizhen Feng, Dongmei Gao, Jieqiong Wang, Chunhong Song, Sheng Wei, Mingqi Qiao
The effects of the Shuyu capsule on 5-HT3AR and 5-HT3BR expression in a rat model of premenstrual syndrome (PMS) depression and on 5-HT3AR and 5-HT3BR expression and hippocampal neuron 5-HT3 channel current were investigated, to elucidate its mechanism of action against PMS depression. PMS depression model rats were divided into depression and Shuyu- and fluoxetine-treated groups, which were compared to control rats for frontal lobe and hippocampal 5-HT3AR and 5-HT3BR expression and behavior. The depressed model rats displayed symptoms of depression, which were reduced in treated and normal control rats...
2016: Neural Plasticity
R Navari
Chemotherapy-induced nausea and vomiting (CINV) is a significant clinical issue which affects patients' quality of life as well as treatment decisions. Significant improvements in the control of CINV have occurred in the past 15 years with the introduction of new antiemetic agents: 5-HT3 receptor antagonists, tachykinin NK1 receptor antagonists and olanzapine. Aprepitant was the first NK1 receptor antagonist introduced (2003) for the prevention of CINV in combination with a 5-HT3 receptor antagonist and dexamethasone...
August 2016: Drugs of Today
H Li, M Diao, J Ni, P Li, Q Zhu, Y L Wan, Y S Ma, X M Lin
BACKGROUND: Serotonin (5-HT) is known to play an important role in regulating uterine contractions. However, the specific receptors involved have not been well characterized. We evaluated whether 5-HT3 receptors exist in human myometrium, and their effects on myometrial contractility when stimulated by a 5-HT3 agonist. METHODS: Four tissue samples taken from patients undergoing hysterectomy (n=2) and elective cesarean delivery (n=2) were used to detect expression of 5-HT3 receptors on the myometrium using western blotting...
September 9, 2016: International Journal of Obstetric Anesthesia
Marta Silva, José Tiago Costa-Pereira, Daniel Martins, Isaura Tavares
Diabetic neuropathy has a profound impact in the quality of life of patients who frequently complain of pain. The mechanisms underlying diabetic neuropathic pain (DNP) are no longer ascribed only to damage of peripheral nerves. The effects of diabetes at the central nervous system are currently considered causes of DPN. Management of DNP may be achieved by antidepressants that act on serotonin (5-HT) uptake, namely specific serotonin reuptake inhibitors. The rostroventromedial medulla (RVM) is a key pain control center involved in descending pain modulation at the spinal cord through local release of 5-HT and plays a peculiar role in the balance of bidirectional control (i...
October 4, 2016: Neurobiology of Disease
Matthew J Erlendson, Nicole D'Arcy, Ellen M Encisco, Jeffrey J Yu, Lorena Rincon-Cruz, Gary Peltz, J David Clark, Larry F Chu
BACKGROUND: Treatments for reducing opioid withdrawal are limited and prone to problematic side effects. Laboratory studies, clinical observations, and limited human trial data suggest 5-HT3-receptor antagonists and antihistamines may be effective. OBJECTIVES: This double-blind, crossover, placebo-controlled study employing an acute physical dependence model evaluated whether (i) treatment with a 5-HT3-receptor antagonist (palonosetron) would reduce opioid withdrawal symptoms, and (ii) co-administration of an antihistamine (hydroxyzine) would enhance any treatment effect...
August 11, 2016: American Journal of Drug and Alcohol Abuse
G Kilciler, M Kilciler, M Kadihasanoglu, O Atahan
Priapism is a rare but severe urological emergency of erection of penis in the absence of physical and psychological sexual stimulation. Priapism is often idiopathic and is commonly associated with medications and underlying medical or traumatic causes. In this report, we present a case of a 70-year-old White Caucasian man who developed priapism after the administration of ondansetron, which is a selective serotonin type-3 (5-HT3) receptor antagonist. This case is unique, because, to date, there are only two presented cases in literature...
October 6, 2016: Andrologia
Deepti Ahuja, Sachidanand J Bharati, Nishkarsh Gupta, Ritesh Kumar, Sushma Bhatnagar
Radiation-induced nausea and vomiting (RINV) is one of the most distressing symptoms that adversely affects quality of life (QOL) as well as the ongoing management plan of cancer patients. Although there are protocols for management of chemotherapy induced nausea and vomiting (CINV) but such guidelines are still lacking for RINV. Various agents like 5-hydroxy tryptophan 3 (5-HT3) antagonist, dexamethasone, metoclopramide and haloperidol are used in clinical practice for RINV but the results are not very encouraging...
August 23, 2016: Annals of Palliative Medicine
Preet Mohinder Singh, Anuradha Borle, Divakara Gouda, Jeetinder Kaur Makkar, Mahesh K Arora, Anjan Trikha, Ashish Sinha, Basavana Goudra
INTRODUCTION: Palonosetron is a second-generation 5-HT3 receptor antagonist with proposed higher efficacy and sustained action for prophylaxis of postoperative nausea and vomiting (PONV). METHODS: Randomized controlled trials involving adult population undergoing elective surgery under general anesthesia comparing palonosetron to placebo, ramosetron, granisetron, and ondansetron were included. Data were extracted for vomiting incidence (VI), complete response (no nausea/vomiting; Complete Response [CR]), and rescue antiemetic need...
November 2016: Journal of Clinical Anesthesia
Andrew D Powell, Gillian Grafton, Alexander Roberts, Shannon Larkin, Nathanael O'Neill, Josephine Palandri, Reka Otvos, Alison J Cooper, Chris Ulens, Nicholas M Barnes
BACKGROUND AND PURPOSE: The 5-HT3 receptor is a prototypical member of the Cys-loop ligand-gated ion channel (LGIC) superfamily and an established therapeutic target. In addition to activation via the orthosteric site, receptor function can be modulated by allosteric ligands. We have investigated the pharmacological action of Cl-indole upon the 5-HT3 A receptor and identified that this positive allosteric modulator possesses a novel mechanism of action for LGICs. EXPERIMENTAL APPROACH: The impact of Cl-indole upon the 5-HT3 receptor was assessed using single cell electrophysiological recordings and [(3) H]granisetron binding with HEK293 cells stably expressing the 5-HT3 receptor...
September 28, 2016: British Journal of Pharmacology
I Mouch, J R B J Brouwers, E van 't Riet, P Nieboer, M H Otten, F G A Jansman
OBJECTIVE: To investigate whether the anti-emetics metoclopramide and domperidone can be replaced by 5-HT3-antagonists, as side effects restrict use of these dopamine antagonists. DESIGN: Systematic review. METHOD: We searched the Embase and PubMed databases for articles published in the period 1995-October 2015, in which the efficacy or side effects of metoclopramide or domperidone were compared with at least one of the 5-HT3-antagonists ondansetron, granisetron, tropisetron or palonosetron...
2016: Nederlands Tijdschrift Voor Geneeskunde
José Ángel García-Pedraza, Mónica García, María Luisa Martín, Nélida Eleno, Asunción Morán
5-hydroxytryptamine (5-HT) modulates the cardiac parasympathetic neurotransmission, inhibiting the bradyarrhythmia by 5-HT2 receptor activation. We aimed to determine whether the chronic selective 5-HT2 blockade (sarpogrelate) could modify the serotonergic modulation on vagal cardiac outflow in pithed rat. Bradycardic responses in rats treated with sarpogrelate (30 mg/; p.o.) were obtained by electrical stimulation of the vagal fibers (3, 6, and 9 Hz) or i.v. injections of acetylcholine (ACh; 1, 5, and 10 μg/kg)...
September 20, 2016: Journal of Cardiovascular Pharmacology
Maurizio S Riga, Vicent Teruel-Martí, Connie Sánchez, Pau Celada, Francesc Artigas
Vortioxetine (VOR) is a multimodal antidepressant drug. VOR is a 5-HT3-R, 5-HT7-R and 5-HT1D-R antagonist, 5-HT1B-R partial agonist, 5-HT1A-R agonist, and serotonin transporter (SERT) inhibitor. VOR shows pro-cognitive activity in animal models and beneficial effects on cognitive dysfunction in major depressive patients. Here we compared the effects of 14-day treatments with VOR and escitalopram (ESC, selective serotonin reuptake inhibitor) on neuronal activity in the medial prefrontal cortex (mPFC). Ten groups of rats (5 standard, 5 depleted of 5-HT with p-chlorophenylalanine -pCPA-, used as model of cognitive impairment) were fed with control food or with two doses of VOR-containing food...
September 23, 2016: Neuropharmacology
Shvetank Bhatt, Radhakrishnan Mahesh, Thangaraj Devadoss, Ankur Jindal
BACKGROUND: 5-HT3 receptor antagonists play a key role in the management of psychiatric disorders such as, depression and anxiety. They may act through modulation of serotonergic transmission. In the present study, a novel and potential 5-HT3 receptor antagonist, 6g (4-benzylpiperazin-1-yl)(3-methoxyquinoxalin-2-yl) methanone, which exhibited good log P (3.08) and pA2 (7.5) values was screened for its anxiolytic property in lipopolysaccharide (LPS) induced anxiety models. METHODS: LPS, an endotoxin, present in the cell wall of Gram negative bacteria was injected 0...
September 24, 2016: Journal of Basic and Clinical Physiology and Pharmacology
Shvetank Bhatt, Radhakrishnan Mahesh, Ankur Jindal, Thangaraj Devadoss
BACKGROUND: Several preclinical studies have shown that serotonergic 5-HT3 receptor antagonists play an important role in the management of neuropsychiatric disorders, such as depression and anxiety. In the present study the compound "6n" (N-n-propyl-3-ethoxyquinoxaline-2-carboxamide), a novel 5-HT3 receptor antagonist with an optimal log P (2.52) and pA2 (7.6) value was screened for its neuro-pharmacological potential in chronic rodent models of depression and anxiety named traumatic brain injury (TBI)...
September 23, 2016: Journal of Basic and Clinical Physiology and Pharmacology
Gerhard G Grabenbauer, Göbel Holger
Possible toxic effects following radiation and chemotherapy of gastrointestinal tumours may cause a depletion of the mucosal barrier within the radiation volumes with severe mucositis. Diarrhoea, nausea, emesis and severe malabsorption followed by infections with dehydration and electrolyte disorders have to be encountered. For prevention and treatment of oropharyngeal mucositis an oral care protocol, oral cryotherapy together with benzydamine mouthwash may be recommended. Lower gastrointestinal diarrhoea is best treated by Octreotide (>100 μg s...
August 2016: Best Practice & Research. Clinical Gastroenterology
Reza Rahimian, Mohammad Reza Zirak, Mojtaba Keshavarz, Nahid Fakhraei, Ahmad Mohammadi-Farani, Hanan Hamdi, Kazem Mousavizadeh
Inflammatory bowel disease (IBD) is a chronic inflammation of the gastrointestinal (GI) tract. Tropisetron, a selective 5-HT3 receptor antagonist, is highly used to counteract chemotherapy-induced emesis. Previous studies revealed the anti-inflammatory properties of this drug. The aim of this study was to evaluate the role of peroxisome proliferator-activated receptor gamma (PPARγ) receptor in the protective effect of tropisetron in an animal model of ulcerative colitis. Experimental colitis was induced by a single intra-colonic instillation of 4% (V/V) acetic acid in male rats...
September 20, 2016: Immunopharmacology and Immunotoxicology
Korinna Ulbricht, Peter Layer, Viola Andresen
Chronic, non-infectious diarrhea can be caused by a variety of gastrointestinal diseases. In anamnesis, it is important to take accompanying warning symptoms and specific triggers into account. The fecal inflammatory marker calprotectin may help differentiating between organic and functional gastrointestinal disorders, but it is not specific. Among other options, gelling fibres, Loperamide and Cholestyramine as well as probiotics are available for the symptomatic treatment of chronic diarrhea. For long-term treatment of chronic diarrhea with the enkephalinase inhibitor racecadotril, which is approved for acute diarrhea, only limited data are available...
September 2016: Deutsche Medizinische Wochenschrift
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