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Kristin Bokelmann, Jürgen Brockmöller, Mladen V Tzvetkov
The organic cation transporter 1 (OCT1, SLC22A1) is strongly expressed in the human liver and facilitates the hepatic uptake of drugs such as morphine, metformin, tropisetron, sumatriptan and fenoterol and of endogenous substances such as thiamine. OCT1 expression is inter-individually highly variable. Here, we analyzed SNPs in the OCT1 promoter concerning their potential contribution to the variability in OCT1 expression. Using electrophoretic mobility shift and luciferase reporter gene assays in HepG2, Hep3B, and Huh7 cell lines, we identified the SNPs -1795G>A (rs6935207) and -201C>G (rs58812592) as having effects on transcription factor binding and/or promoter activity...
December 11, 2018: Journal of Personalized Medicine
Zhengjiang Liu, Zhiheng Zeng, Changdong Wu, Hua Liu
OBJECTIVE: The objective of the present investigation was to explore the possible effect of the 5-HT3 receptor antagonist tropisetron on the expression levels of the inflammatory factors interleukin 6 (IL-6), creatine kinase isoenzyme (CK-MB), soluble growth stimulating gene 2 protein (sST2) and immunoglobulin E (IgE), as well as the cardiac action potential in septic rats. METHODS: The cecal ligation and perforation (CLP) method was utilized to construct abdominal infarction in rats...
December 4, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Jorinde Aw Polderman, Violet Farhang-Razi, Susan Van Dieren, Peter Kranke, J Hans DeVries, Markus W Hollmann, Benedikt Preckel, Jeroen Hermanides
BACKGROUND: In the perioperative period, dexamethasone is widely and effectively used for prophylaxis of postoperative nausea and vomiting (PONV), for pain management, and to facilitate early discharge after ambulatory surgery.Long-term treatment with steroids has many side effects, such as adrenal insufficiency, increased infection risk, hyperglycaemia, high blood pressure, osteoporosis, and development of diabetes mellitus. However, whether a single steroid load during surgery has negative effects during the postoperative period has not yet been studied...
November 23, 2018: Cochrane Database of Systematic Reviews
Lucie Polovinkin, Ghérici Hassaine, Jonathan Perot, Emmanuelle Neumann, Anders A Jensen, Solène N Lefebvre, Pierre-Jean Corringer, Jacques Neyton, Christophe Chipot, Francois Dehez, Guy Schoehn, Hugues Nury
The serotonin 5-HT3 receptor is a pentameric ligand-gated ion channel (pLGIC). It belongs to a large family of receptors that function as allosteric signal transducers across the plasma membrane1,2 ; upon binding of neurotransmitter molecules to extracellular sites, the receptors undergo complex conformational transitions that result in transient opening of a pore permeable to ions. 5-HT3 receptors are therapeutic targets for emesis and nausea, irritable bowel syndrome and depression3 . In spite of several reported pLGIC structures4-8 , no clear unifying view has emerged on the conformational transitions involved in channel gating...
November 2018: Nature
Shasha Guan, Lisha Zhang, Diansheng Zhong, Qing Ma, Fanlu Meng, Yi Shao, Tao Yu, Xia Liu
BACKGROUND: Chemotherapy is the most important method for cancer treatment. However, chemotherapy induced nausea and vomiting (CINV) has a profound effect on patients. In recent years, there have been new antiemetic drugs, such as aprepitant. We review the curative effect of aprepitant with tropisetron and dexamethasone for prevention of nausea and vomiting in patients receiving Cisplatin chemotherapy. METHODS: Observation is divided into three stages. Whole study phase (0-120 h after chemotherapy administration), acute phases (0-24 h), and delayed phase (24 h-120 h)...
October 20, 2018: Zhongguo Fei Ai za Zhi, Chinese Journal of Lung Cancer
Jorinde Aw Polderman, Violet Farhang-Razi, Susan Van Dieren, Peter Kranke, J Hans DeVries, Markus W Hollmann, Benedikt Preckel, Jeroen Hermanides
BACKGROUND: In the perioperative period, dexamethasone is widely and effectively used for prophylaxis of postoperative nausea and vomiting (PONV), for pain management, and to facilitate early discharge after ambulatory surgery.Long-term treatment with steroids has many side effects, such as adrenal insufficiency, increased infection risk, hyperglycaemia, high blood pressure, osteoporosis, and development of diabetes mellitus. However, whether a single steroid load during surgery has negative effects during the postoperative period has not yet been studied...
August 28, 2018: Cochrane Database of Systematic Reviews
H W Wang, L L Li, Z S Li, L N Cheng
Objective: To evaluate the safety and efficiency of patient-controlled intravenous analgesia (PCIA) using hydromorphone supplement with dexmedetomidine on patients undergoing transcatheter arterial chemoembolization. Methods: One hundred and eighty patients, age ranged from 40 to 65 years, body mass index from 18 to 25 kg/m(2,) ASA physical status Ⅱ-Ⅲ, who were scheduled for transcatheter arterial chemoembolization (TACE) under monitor anesthesia care (MAC) were randomly divided into 3 groups: hydromorphone group (H group), hydromorphone supplement with dexmedetomidine 1 μg/kg group (D1 group), hydromorphone supplement with dexmedetomidine 2 μg/kg group (D2 group), 60 patients in every group...
August 23, 2018: Zhonghua Zhong Liu za Zhi [Chinese Journal of Oncology]
Cunying Huang, Huihui Wan, Jing Zhang, Hongmin Zhong, Juan Li, YuMing Sun, Qing Wang, Hua Zhang
An assay method to quantify ondansetron (OND), granisetron (GRA) and tropisetron (TRO) in goat plasma has been successfully developed and validated. This method procedure for the analysis of OND, GRA and TRO was involved of extracting samples with hydrophilic interaction liquid chromatography (HILIC) solid phase extraction (SPE) and determination by liquid chromatography coupled to tandem mass spectroscopy. An SPE method for the simultaneous extraction of OND, GRA and TRO with high efficiency and selectivity was developed...
September 15, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Wen Kou, Hongyan Qin, Shahbaz Hanif, Xinan Wu
Objective: 5-HT3 receptor antagonist (ondansetron) has been reported to have nephrotoxic effect when combined with cisplatin in mice; however, little evidence exists in explaining its nephrotoxic effects on patients. The aim of this present study was to investigate whether 5-HT3 receptor antagonist could enhance or aggravate the incidence of cisplatin-induced nephrotoxicity in patients. Methods: We retrospectively reviewed 600 tumor patients which were treated with cisplatin ( ⩾ 60 mg/m2 ) as a first-time chemotherapy and combined with 5-HT3 receptor antagonist (i...
2018: BioMed Research International
Glaucia Tobaldini, Natalia F Sardi, Vinicius A Guilhen, Luana Fischer
The ability to modulate pain perception is as critical to survival as pain itself. The most known pain modulation pathway is the PAG-RVM (periaqueductal gray-rostral ventromedial medulla) descending system. In this study, we hypothesized that it is functionally linked to the ascending nociceptive control, which is a form of pain-induced analgesia dependent on mesolimbic mechanisms. To test this hypothesis, we used a pharmacological approach, in which the antinociception induced by noxious stimulation (forepaw injection of capsaicin) was detected in a standard rat model of inflammatory pain (hindpaw injection of carrageenan)...
June 1, 2018: Molecular Neurobiology
Yan Yu, Wanhu Zhu, Qing Liang, Jing Liu, Xu Yang, Guangchun Sun
Tropisetron, an antagonist of serotonin type 3 receptors (5-HT3 Rs), has been investigated in colonic inflammatory process. Since substance P/neurokinin 1 receptor (SP/NK1R) signaling pathway plays a key role in several sensory neuronal inflammatory. We evaluated the anti-inflammatory activity of tropisetron in mice cerebral cortex, and discovered that it was a potential inhibitor in LPS-mediated neuron inflammation through SP/NK1R signaling pathway. We found that tropisetron significantly reduced the increased number of iba-1 positive microglia, down-regulated the gene transcription and protein expression of IL-1β,IL-6 and TNF-α in LPS stimulated cerebral cortex...
July 15, 2018: Journal of Neuroimmunology
Quanfu Li, Wenjuan Wang, Gang Chen, Shuqin Deng, Caihong Jiang, Feng Chen, Jun Zhao, Hui Li, Xiaojun Bai, Yuliang Hu, Lenggaowa Da, Yungaowa Wu, Gaowa Jin
Objective: To perform a prospective non-randomized comparison of the effectiveness and safety of combined neurokinin-1 antagonist aprepitant treatment with the standard multiple-day cisplatin regimen for the prevention of cisplatin-induced nausea and vomiting (CINV). Methods: Patients being administered 3-day cisplatin-based chemotherapy (25 mg/m2 /d) who had never received aprepitant were given either the standard regimen (tropisetron and dexamethasone) or the aprepitant regimen (aprepitant plus tropisetron and dexamethasone)...
2018: Open Medicine (Warsaw, Poland)
Z-Y Yao, Z Jia, Y-H Xie, L-L Zhang, H-S Zhang, W-Q Wu, C-K Zhang, L-J Gan
OBJECTIVE: To study the analgesic effect of dezocine in different doses on elderly patients undergoing abdominal operation under general anesthesia and to investigate the influence of dezocine on stress response to postoperative tracheal extubation. PATIENTS AND METHODS: A total of 76 elderly patients undergoing abdominal operation under general anesthesia and postoperative analgesia in our hospital from January 2015 to January 2016 were selected, and patients treated with fentanyl were selected as the control group (fentanyl: 10 μg/kg, n=19)...
November 2017: European Review for Medical and Pharmacological Sciences
Indrani Poddar, Patrick M Callahan, Caterina M Hernandez, Xiangkun Yang, Michael G Bartlett, Alvin V Terry
While impairments of cognition in schizophrenia have the greatest impact on long-term functional outcome, the currently prescribed treatments, antipsychotic drugs (APDs), do not effectively improve cognition. Moreover, while more than 20 years have been devoted to the development of new drugs to treat cognitive deficits in schizophrenia, none have been approved to date. One area that has not been given proper attention at the preclinical or clinical stage of drug development is the chronic medication history of the test subject...
May 2018: Biochemical Pharmacology
Ya-Xin Liu, Zhi-Fei Wang, Yan-Ming Xie, Yin Zhang, Cen Chen, Yan Zhuang
To analyze the clinical application features of Fufang Kushen injection in treating malignant esophageal tumors in the real world by using hospital information system database, and provide reference for clinical application of Fufang Kushen injection. The electronic medical data from 2 550 patients with malignant esophageal tumors using Fufang Kushen injection from 22 large-scale hospitals nationwide were extracted based on the hospital information system (HIS) established by Institute of Basic Research in Clinical Medicine, China Academy of Chinese Medical Sciences...
August 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
N Humblot, N Thiriet, S Gobaille, D Aunis, J Zwiller
Transcription regulatory factors are rapidly induced in brain by a wide variety of stimuli and may be important in coordinating changes in gene expression underlying neuronal plasticity. Using in situ hybridization, we found that acute cocaine administration (20 mg/kg, intraperitoneally (i.p.)) produced a robust induction of both c-fos and egr-1 immediate early genes. Egr-1 messenger RNA induction was highest in the caudate putamen and in the shell of the nucleus accumbens. No significant induction was noticed after injection of fluoxetine, a selective inhibitor of serotonin uptake...
May 1998: Annals of the New York Academy of Sciences
Sha Li, Man Zheng, Wenzhong Wu, Jie Guo, Fangbin Ji, Zhen Zheng
OBJECTIVE: Our study aimed to investigate the feasibility and effectiveness of preoperative electroacupuncture (EA), delivered 24hours before surgery, on postoperative nausea and vomiting (PONV) and postoperative pain in patients undergoing gynecologic laparoscopic surgery. METHODS: In this randomized controlled trial, 40 patients scheduled for elective gynecologic laparoscopic surgery were randomly assigned to the usual care (UC) group and the EA group (n = 20 each)...
September 2017: Explore: the Journal of Science and Healing
Reza Rahimian, Mohammad Reza Zirak, Mohammad Seyedabadi, Mojtaba Keshavarz, Amir Rashidian, Sareh Kazmi, Amir Hossein Jafarian, Gholamreza Karimi, Kazem Mousavizadeh
Acute pancreatitis (AP) causes morbidity and mortality. The aim of the present study was to investigate the protective effect of tropisetron against AP induced by cerulein. Cerulein (50μg/kg, 5 doses) was used to induce AP in mice. Six hours after final cerulein injection, animals were decapitated. Hepatic/pancreatic enzymes in the serum, pancreatic content of malondialdehyde (MDA), pro-inflammatory cytokines and myeloperoxidase (MPO) activity were measured. Tropisetron significantly attenuated pancreatic injury markers and decreased the amount of elevated serum amylase, lipase, alanine aminotransferase (ALT), aspartate aminotransferase (AST), MPO activities and pro-inflammatory cytokines levels caused by AP in mice...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Nissar A Darmani, Seetha Chebolu, Weixia Zhong, William D Kim, Matthew Narlesky, Joia Adams, Fanglong Dong
The introduction of second generation serotonin 5-HT3 receptor (5-HT3 ) antagonist palonosetron combined with long-acting substance P neurokinin NK1 receptor (NK1 ) antagonists (e.g. netupitant) has substantially improved antiemetic therapy against early- and delayed-phases of emesis caused by highly emetogenic chemotherapeutics such as cisplatin. However, the improved efficacy comes at a cost that many patients cannot afford. We introduce a new class of antiemetic, the antiasthmatic leukotriene CysLT1 receptor antagonist pranlukast for the suppression of cisplatin-evoked vomiting...
August 15, 2017: European Journal of Pharmacology
Saeed Amiri Gheshlaghi, Razieh Mohammad Jafari, Mohammad Algazo, Nastaran Rahimi, Hussein Alshaib, Ahmad Reza Dehpour
Genistein, a major source of phytoestrogen exposure for humans and animals, has been shown to mediate neuroprotection in Alzheimer's disease and status epilepticus. In the present study, we investigated the effect of genistein on pentylenetetrazole-induced seizures in ovariectomized mice and the possible involvement of estrogenic and serotonergic pathways in the probable effects of genistein. Intraperitoneal (i.p.) administration of genistein (10 mg/kg) significantly increased the seizure threshold 30 min prior to induction of seizures 14 days after ovariectomy surgery...
July 2017: Journal of Natural Medicines
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