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https://www.readbyqxmd.com/read/29430989/nk1r-5-ht1ar-interaction-is-related-to-the-regulation-of-melanogenesis
#1
Huali Wu, Yucheng Zhao, Qiaoling Huang, Minxuan Cai, Qi Pan, Mengsi Fu, Xiaohong An, Zhenjiang Xia, Meng Liu, Yu Jin, Ling He, Jing Shang
Substance P (SP) is a candidate mediator along the brain-skin axis and can mimic the effects of stress to regulate melanogenesis. Previously, we and others have found that the regulation of SP for pigmentary function was mediated by neurokinin 1 receptor (NK1R). Emerging evidence has accumulated that psychologic stress can induce dysfunction in the cutaneous serotonin 5-hydroxytryptamine (5-HT)-5-HT1A/1B receptor system, thereby resulting in skin hypopigmentation. Moreover, NK1R and 5-HTR (except 5-HT3) belong to GPCR...
February 7, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29413286/radiation-dose-to-the-thoracic-vertebral-bodies-is-associated-with-acute-hematologic-toxicities-in-patients-receiving-concurrent-chemoradiation-for-lung-cancer-results-of-a-single-center-retrospective-analysis
#2
Christian L Barney, Nicholas Scoville, Eric Allan, Ahmet Ayan, Dominic DiCostanzo, Karl E Haglund, John Grecula, Terence Williams, Meng Xu-Welliver, Gregory A Otterson, Jose G Bazan
PURPOSE: To test the hypothesis that increasing radiation therapy (RT) dose to the thoracic vertebral bodies (TVBs) contributes to the development of hematologic toxicities (HTs) in patients with lung cancer. METHODS AND MATERIALS: Cases of non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) treated with definitive chemoradiation with concurrent platinum-based doublet chemotherapy at our institution from 2007 to 2016 were identified. Mean TVB dose and the volume of TVBs receiving at least 5 to 60 Gy (V 5 -V 60 ) were retrospectively recorded...
March 1, 2018: International Journal of Radiation Oncology, Biology, Physics
https://www.readbyqxmd.com/read/29412172/in-vitro-pharmacology-of-ambroxol-potential-serotonergic-sites-of-action
#3
J D Hull, R A Lyon
AIMS: Ambroxol is a muco-active agent with multiple, clinically relevant effects in the airway. Despite its widespread use and well documented clinical efficacy, there are few data on its mechanism of action and receptor pharmacology beyond sodium channel blockade and inhibition of guanylate cyclase. Accordingly, in vitro studies were conducted to determine its overall receptor pharmacology and possible sites of action. MATERIALS AND METHODS: In vitro radioligand binding/enzyme inhibition studies were conducted at 62 receptors, ion channels and enzymes using standard techniques...
February 2, 2018: Life Sciences
https://www.readbyqxmd.com/read/29407728/strain-differences-in-the-development-of-cisplatin-induced-pica-behavior-in-mice
#4
Kouichi Yamamoto, Atsushi Yamatodani
INTRODUCTION: Pica behavior, kaolin ingestion, in rats and mice can be used as an assessment of nausea and vomiting; however, we observed that the incidence of pica behavior in ICR strain mice varied markedly. We investigated the susceptibility of four strains of mice (ICR, BALB/c, C57BL/6, and DBA/2) to the development of pica behavior. METHODS: Mice received cisplatin (7.5 mg/kg, i.p.) with or without a serotonin 5-HT3 receptor antagonist (granisetron: 0.1 mg/kg, i...
January 30, 2018: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/29385389/compatibility-and-stability-of-varubi-rolapitant-injectable-emulsion-admixed-with-intravenous-granisetron-hydrochloride
#5
George Wu, Dan Powers, Stanley Yeung, Frank Chen, Kelly Neelon
Prophylaxis or therapy with a combination of a neurokinin 1 (NK-1) receptor antagonist (RA), a 5-hydroxytryptamine- 3 (5-HT3) RA, and dexamethasone is recommended by international antiemesis guidelines for the prevention of chemotherapy-induced nausea and vomiting for patients receiving highly emetogenic chemotherapy and for select patients receiving moderately emetogenic chemotherapy. VARUBI (rolapitant) is a substance P/NK-1 RA that was recently approved by the U.S. Food and Drug Administration as an injectable emulsion in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy...
January 2018: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/29385388/compatibility-and-stability-of-varubi-rolapitant-injectable-emulsion-admixed-with-intravenous-palonosetron-hydrochloride-injection-and-dexamethasone-sodium-phosphate-injection
#6
George Wu, Dan Powers, Stanley Yeung, Frank Chen
Prophylaxis or therapy with a combination of a neurokinin 1 (NK-1) receptor antagonist (RA), a 5-hydroxytryptamine-3 (5-HT3) RA, and dexamethasone is recommended by international antiemesis guidelines for the prevention of chemotherapy-induced nausea and vomiting for patients receiving highly emetogenic chemotherapy and for selected patients receiving moderately emetogenic chemotherapy. VARUBI (rolapitant) is a substance P/NK-1 RA that was recently approved by the U.S. Food and Drug Administration as an injectable emulsion in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy...
January 2018: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/29369737/pharmacology-of-serotonin-receptors-causing-contraction-of-isolated-bovine-posterior-ciliary-arteries-role-in-ocular-blood-flow
#7
Ya Fatou Njie-Mbye, Jenaye Robinson, Leah Mitchell-Bush, Marshalyn Mckoy, Catherine A Opere, Sunny E Ohia, Naj Sharif
PURPOSE: To determine the serotonergic (5HT) receptor subtype mediating the contraction of bovine posterior ciliary arteries (BPCAs) in vitro. METHODS: Longitudinal isometric tension was measured in BPCA strips (4-5 mm) mounted in 25 mL organ baths containing oxygenated Krebs solution at 37°C. Cumulative contractile concentration-response (C-R) curves were generated for various 5-HT agonists to assess their potencies and maximal degrees of contraction. Multiple agonist C-R curves were also constructed in the presence and absence of receptor-selective antagonists to determine antagonist potencies using Schild plots...
January 25, 2018: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29362306/-evaluation-of-chemotherapy-induced-nausea-and-vomiting-in-patients-with-hematological-malignancies-using-mascc-antiemesis-tool-mat
#8
Kana Oiwa, Naoko Hosono, Kazuhiro Itoh, Miyuki Ookura, Yasufumi Matsuda, Katsunori Tai, Takanori Ueda, Takahiro Yamauchi
Chemotherapy-induced nausea and vomiting(CINV)were prospectively evaluated using MASCC Antiemesis Tool(MAT) in patients with hematological malignancies in our institution. A total of 33 patients receiving 46 chemotherapy courses were evaluated. Although vomiting was not observed in the acute phase, nausea was seen in 22.6% and 32.3% of the patients in the acute and delayed phases, respectively. Thirty percent(25 cases)of the patients receiving highly emetogenic chemotherapy presented nausea in both the phases, while 40%(18 cases)of the patients receiving moderately emetogenic chemotherapy presented nausea in the delayed phase...
January 2018: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/29345696/antiemetic-efficacy-and-safety-of-granisetron-or-palonosetron-alone-and-in-combination-with-a-corticosteroid-for-abvd-therapy-induced-nausea-and-vomiting
#9
Mayako Uchida, Tsutomu Nakamura, Kojiro Hata, Hiroyuki Watanabe, Yasuo Mori, Koji Kato, Kenjiro Kamezaki, Katsuto Takenaka, Motoaki Shiratsuchi, Keiko Hosohata, Toshihiro Miyamoto, Koichi Akashi
Background: Antiemetic effects and safety of granisetron or palonosetron alone and in combination with a corticosteroid against chemotherapy-induced nausea and vomiting (CINV) were retrospectively evaluated in patients with Hodgkin lymphoma receiving adriamycin, bleomycin, vinblastine, and dacarbazine (ABVD) therapy. Methods: A total of 39 patients were eligible for this study. Before ABVD therapy, granisetron or palonosetron was intravenously administered with or without a corticosteroid (dexamethasone or hydrocortisone) and aprepitant...
2018: Journal of Pharmaceutical Health Care and Sciences
https://www.readbyqxmd.com/read/29326489/ondansetron-ameliorates-depression-associated-with-obesity-in-high-fat-diet-fed-experimental-mice-an-investigation-based-on-the-behavioral-biochemical-and-molecular-approach
#10
Yeshwant Kurhe, Radhakrishnan Mahesh
INTRODUCTION: Obesity is an important risk factor for depression as more than half of the obese population is susceptible for depression at double rate. Our earlier studies reported the antidepressant potential of 5-HT3 receptor antagonist, ondansetron (OND) in depression associated obesity using behavioral tasks. The present research work is aimed to evaluate the effect of OND on depression associated with obesity with special emphasis on biochemical and molecular mechanisms such as hippocampal brain-derived neurotrophic factor (BDNF), cyclic adenosine monophosphate (cAMP), 5-hydroxytryptamine (5-HT), hippocampal histological examination and immunohistochemical expression of p53 proteins...
July 2017: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/29313107/treatment-possibilities-for-low-anterior-resection-syndrome-a-review-of-the-literature
#11
REVIEW
Audrius Dulskas, Edgaras Smolskas, Inga Kildusiene, Narimantas E Samalavicius
AIM: Up to 80% of patients after low anterior resection, experience (low) anterior resection syndrome (ARS/LARS). However, there is no standard treatment option currently available. This systemic review aims to summarize treatment possibilities for LARS after surgical treatment of rectal cancer in the medical literature. METHODS: Embase, PubMed, and the Cochrane Library were searched using the terms anterior resection syndrome, low anterior resection, colorectal/rectal/rectum, surgery/operation, pelvic floor rehabilitation, biofeedback, transanal irrigation, sacral nerve stimulation, and tibial nerve stimulation...
January 8, 2018: International Journal of Colorectal Disease
https://www.readbyqxmd.com/read/29310827/meta-analysis-of-safety-and-efficacy-of-rolapitant-nk-1-receptor-antagonist-for-prevention-of-chemotherapy-induced-nausea-and-vomiting
#12
REVIEW
Hussien Ahmed, Ali Mohamed Hammad, Abdelrahman Ibrahim Abushouk, Mohamed Zidan, Mohamed Salem, Ahmed Negida, Mohamed M Abdel-Daim
Although chemotherapeutic agents represent a cornerstone of cancer treatment, chemotherapy-induced nausea and vomiting (CINV) affect the patients' quality of life and basic daily activities. Rolapitant is a novel selective neurokinin-1 receptor antagonist (NK-1 RA), which was clinically approved for prevention of CINV. The aim of the present study is to synthesize evidence about the safety and efficacy of rolapitant in combination with other antiemetic agents for prophylaxis against CINV. We performed a web-based literature search of six authentic databases to identify eligible studies...
December 6, 2017: Current Problems in Cancer
https://www.readbyqxmd.com/read/29298898/a-triad-of-residues-is-functionally-transferrable-between-5-ht3-serotonin-receptors-and-nicotinic-acetylcholine-receptors
#13
Richard Mosesso, Dennis A Dougherty
Cys-loop receptors are pentameric ligand-gated ion channels that facilitate communication within the nervous system. Upon neurotransmitter binding, these receptors undergo an allosteric activation mechanism connecting the binding event to the membrane-spanning channel pore, which expands to conduct ions. Some of the earliest steps in this activation mechanism are carried out by residues proximal to the binding site, the relative positioning of which may reflect functional differences among members of the Cys-loop family of receptors...
January 3, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29284389/efficacy-and-safety-of-serotonin-receptor-ligands-in-the-treatment-of-irritable-bowel-syndrome-a-review
#14
Agata Binienda, Martin Storr, Jakub Fichna, Maciej Salaga
Irritable bowel syndrome (IBS) is a chronic, recurrent bowel disorder with an unknown etiology, which is most likely multifactorial. Increased mucosal permeability, visceral hypersensitivity and activation status of intestinal mucosal immune cells cause changes in gastrointestinal (GI) motility, secretion and sensation observed in the course of IBS. Permanent, cumbersome symptoms, such as diarrhea, constipation and abdominal pain greatly lower quality of life of IBS patients. On this basis, according to the Rome IV criteria, different forms of IBS can be distinguished...
December 27, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29280949/peripheral-5-ht3-receptors-are-involved-in-the-antinociceptive-effect-of-bunodosine-391
#15
Wilson Alves Ferreira Junior, Andre Junqueira Zaharenko, Kohei Kazuma, Gisele Picolo, Vanessa Pacciari Gutierrez, Jose Carlos de Freitas, Katsuhiro Konno, Yara Cury
Bunodosine 391 (BDS 391), a low molecular weight compound isolated from the sea anemone Bunodosoma cangicum, increases the nociceptive threshold and inhibits inflammatory hyperalgesia. Serotonin receptors are involved in those effects. In this study, we have expanded the characterization of the antinociceptive effect of BDS 391 demonstrating that, in rats: (a) the compound inhibits (1.2-12 ng/paw) overt pain, in the formalin test, and mechanical hyperalgesia (0.6-6.0 ng/paw) detected in a model of neuropathic pain; (b) intraplantar administration of ondansetron, a selective 5-HT3 receptor antagonist, blocks the effect of BDS 391, whereas ketanserin, a 5-HT2 receptor antagonist, partially reversed this effect, indicating the involvement of peripheral 5-HT2 and 5-HT3 receptors in BDS 391 antinociception; and (c) in binding assay studies, BDS 391 was not able to displace the selective 5-HT receptor antagonists, suggesting that this compound does not directly bind to these receptors...
December 27, 2017: Toxins
https://www.readbyqxmd.com/read/29277715/direct-modification-of-the-5-ht3-receptor-current-by-some-anticancer-drugs
#16
Yukiko Nakamura, Yusuke Ishida, Makoto Kondo, Shoichi Shimada
The serotonin (5-hydroxytryptamine) type 3 (5-HT3) receptor is an important target in the control of emesis, and 5-HT3 receptor antagonists are effective against the early phase chemotherapy evoked vomiting. We recently reported that the anticancer drugs irinotecan and topotecan directly modulate the 5-HT-mediated 5-HT3 receptor current in vitro. In addition, the drug response depends on the 5-HT3 subunit composition. Here, we explored the effects of 35 anticancer drugs on the 5-HT3 receptor current. We microinjected Xenopus laevis oocytes with human 5-HT3A cRNA or a combination of human 5-HT3A and human 5-HT3B cRNA, and performed two-electrode voltage clamp recordings of 5-HT3A and 5-HT3AB receptor currents in the presence of each of the 35 drugs...
December 22, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29274875/the-multimodal-antidepressant-vortioxetine-may-facilitate-pyramidal-cell-firing-by-inhibition-of-5-ht3-receptor-expressing-interneurons-an-in-vitro-study-in-rat-hippocampus-slices
#17
Elena Dale, Morten Grunnet, Alan L Pehrson, Kristen Frederiksen, Peter H Larsen, Jacob Nielsen, Tine B Stensbøl, Bjarke Ebert, Haolan Yin, Dunguo Lu, Huiquing Liu, Thomas N Jensen, Charles R Yang, Connie Sanchez
The multimodal antidepressant vortioxetine is thought to mediate its pharmacological effects via 5-HT1A receptor agonism, 5-HT1B receptor partial agonism, 5-HT1D, 5-HT3, 5-HT7 receptor antagonism and 5-HT transporter inhibition. Here we studied vortioxetine's functional effects across species (canine, mouse, rat, guinea pig and human) in cellular assays with heterologous expression of 5-HT3A receptors (in Xenopus oocytes and HEK-293 cells) and in mouse neuroblastoma N1E-115 cells with endogenous expression of 5-HT3A receptors...
December 21, 2017: Brain Research
https://www.readbyqxmd.com/read/29273459/mirtazapine-impairs-acquisition-and-reinstatement-of-cocaine-induced-place-preference-in-rats
#18
Susana Barbosa-Méndez, Maura Matus-Ortega, Salomón Jacinto-Gutiérrez, Alberto Salazar-Juárez
Exposure to cues previously associated with drug use and the environment can trigger intense craving and drug-seeking, often leading to relapse in individuals with substance use disorders. Several studies suggest that the decrease in the effects of the cues and the environment could help maintain abstinence from drug use in individuals abusing drugs. Mirtazapine, an antagonist of the noradrenergic (NE) α2 receptor and the 5-HT2A/C and 5-HT3 receptors has demonstrated efficacy in reducing the rewarding effect of different drugs...
December 19, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29245992/htr3a-and-htr3e-gene-polymorphisms-and-diarrhea-predominant-irritable-bowel-syndrome-risk-evidence-from-a-meta-analysis
#19
Tangming Guan, Ting Li, Weiming Cai, Dong Huang, Peipei Ouyang, Yan Wang, Huayan Chen, Kefeng Wu, Xiaoli Ma
Several studies have reported an association between serotonin receptor type 3 (5-HT3) subunit genes HTR3A (rs1062613) and HTR3E (rs62625044) and diarrhea predominant irritable bowel syndrome (IBS-D). However, the results remain inconclusive and controversial, particularly for the data derived from different ethnicities and genders. Therefore, we performed a meta-analysis to evaluate this association. All eligible case-control studies that met the search criteria were retrieved from multiple databases, and five case-control studies were included for detailed evaluation...
November 21, 2017: Oncotarget
https://www.readbyqxmd.com/read/29244998/applicability-of-the-national-comprehensive-cancer-network-multinational-association-of-supportive-care-in-cancer-guidelines-for-prevention-and-management-of-chemotherapy-induced-nausea-and-vomiting-in-southeast-asia-a-consensus-statement
#20
Alexandre Chan, Matin M Abdullah, Wan Zamaniah B Wan Ishak, Annielyn B Ong-Cornel, Antonio H Villalon, Ravindran Kanesvaran
A meeting of regional experts was convened in Manila, Philippines, to develop a resource-stratified chemotherapy-induced nausea and vomiting (CINV) management guideline. In patients treated with highly emetogenic chemotherapy in general clinical settings, triple therapy with a serotonin (5-hydroxytryptamine-3 [5-HT3]) antagonist (preferably palonosetron), dexamethasone, and aprepitant is recommended for acute CINV prevention. In resource-restricted settings, triple therapy is still recommended, although a 5-HT3 antagonist other than palonosetron may be used...
December 2017: Journal of Global Oncology
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