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https://www.readbyqxmd.com/read/27910986/catalytic-photodegradation-of-pharmaceuticals-homogeneous-and-heterogeneous-photocatalysis
#1
S Klementova, D Kahoun, L Doubkova, K Frejlachova, M Dusakova, M Zlamal
Photocatalytic degradation of pharmaceuticals (hydrocortisone, estradiol, and verapamil) and personal care product additives (parabens-methyl, ethyl, and propyl derivatives) was investigated in the homogeneous phase (with ferric ions as the catalyst) and on TiO2. Ferric ions in concentrations corresponding to concentrations in natural water bodies were shown to be a significant accelerator of the degradation in homogeneous reaction mixtures. In heterogeneous photocatalytic reactions on TiO2, lower reaction rates, but mineralisation to higher extents, were observed...
December 2, 2016: Photochemical & Photobiological Sciences
https://www.readbyqxmd.com/read/27905406/differential-roles-for-l-type-calcium-channel-subtypes-in-alcohol-dependence
#2
Stefanie Uhrig, David Vandael, Andrea Marcantoni, Nina Dedic, Ainhoa Bilbao, Miriam A Vogt, Natalie Hirth, Laura Broccoli, Rick E Bernardi, Kai Schönig, Peter Gass, Dusan Bartsch, Rainer Spanagel, Jan M Deussing, Wolfgang H Sommer, Emilio Carbone, Anita C Hansson
It has previously been shown that the inhibition of L-type calcium channels (LTCCs) decreases alcohol consumption, although the contribution of the central LTCC subtypes Cav1.2 and Cav1.3 remains unknown. Here, we determined changes in Cav1.2 (Cacna1c) and Cav1.3 (Cacna1d) mRNA and protein expression in alcohol dependent rats during protracted abstinence and naïve controls using in situ hybridization and Western Blot analysis. Functional validation was obtained by electrophysiological recordings of calcium currents in dissociated hippocampal pyramidal neurons...
December 1, 2016: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27899939/beta-blocker-use-and-risk-of-symptomatic-bradyarrhythmias-a-hospital-based-case-control-study
#3
Hou Tee Lu, Jiyen Kam, Rusli Bin Nordin, Surinder Kaur Khelae, Jing Mein Wang, Chun Ngok Choy, Chuey Yan Lee
OBJECTIVE: To investigate the risk factors of symptomatic bradyarrhythmias in relation to β-blockers use. METHODS: A hospital-based case-control study [228 patients: 108 with symptomatic bradyarrhythmias (cases) and 120 controls] was conducted in Sultanah Aminah Hospital, Malaysia between January 2011 and January 2014. RESULTS: The mean age was 61.1 ± 13.3 years with a majority of men (68.9%). Cases were likely than control to be older, hypertensive, lower body mass index and concomitant use of rate-controlling drugs (such as digoxin, verapamil, diltiazem, ivabradine or amiodarone)...
September 2016: Journal of Geriatric Cardiology: JGC
https://www.readbyqxmd.com/read/27898257/assessment-of-nifedipine-therapy-in-hyperinsulinemic-hypoglycemia-due-to-mutations-in-the-abcc8-gene
#4
M Güemes, P Shah, S Silvera, K Morgan, C Gilbert, L Hinchey, K Hussain
CONTEXT: Previous case reports have documented the effectiveness of L-type calcium channel blockers (such as Nifedipine and Verapamil) for treating different forms of hyperinsulinemic hypoglycemia (HH). OBJECTIVE: To systematically assess the glycemic response to Nifedipine therapy in 11 patients with HH due to mutations in the ABCC8 gene. DESIGN: Dose escalation of Nifedipine therapy Setting: Inpatients at a tertiary hospital Patients or Other Participants: 11 children with diazoxide unresponsive HH due to mutations in the ABCC8 gene...
November 29, 2016: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/27890480/chemerin-induced-arterial-contraction-is-gi-and-calcium-dependent
#5
David J Ferland, Emma S Darios, Richard R Neubig, Benita Sjögren, Nguyen Truong, Rosa Torres, Thomas S Dexheimer, Janice M Thompson, Stephanie W Watts
Chemerin is an adipokine associated with increased blood pressure, and may link obesity with hypertension. We tested the hypothesis that chemerin-induced contraction of the vasculature occurs via calcium flux in smooth muscle cells. Isometric contraction of rat aortic rings was performed in parallel with calcium kinetics of rat aortic smooth muscle cells to assess the possible signaling pathway. Chemerin-9 (nonapeptide of the chemerin S(157) isoform) caused a concentration-dependent contraction of isolated aorta (EC50 100nM) and elicited a concentration-dependent intracellular calcium response (EC50 10nM)...
November 24, 2016: Vascular Pharmacology
https://www.readbyqxmd.com/read/27887024/insulinoma-or-non-insulinoma-pancreatogenous-hypoglycemia-a-diagnostic-dilemma
#6
Blaire Anderson, Jordan Nostedt, Safwat Girgis, Tara Dixon, Veena Agrawal, Edward Wiebe, Peter A Senior, A M James Shapiro
Insulinoma is the most common cause of endogenous hyperinsulinemic hypoglycemia in adults. An alternate etiology, non-insulinoma pancreatogenous hypoglycemia (NIPH), is rare. Clinically, NIPH is characterized by postprandial hyperinsulinemic hypoglycemia, negative 72-h fasts, negative preoperative localization studies for insulinoma and positive selective arterial calcium infusion tests. Histologically, diffuse islet hyperplasia with increased number and size of islet cells is present and confirms the diagnosis...
November 24, 2016: Journal of Surgical Case Reports
https://www.readbyqxmd.com/read/27886150/improvement-of-transmembrane-transport-mechanism-study-of-imperatorin-on-p-glycoprotein-mediated-drug-transport
#7
Zheng-Gen Liao, Tao Tang, Xue-Jing Guan, Wei Dong, Jing Zhang, Guo-Wei Zhao, Ming Yang, Xin-Li Liang
P-glycoprotein (P-gp) affects the transport of many drugs; including puerarin and vincristine. Our previous study demonstrated that imperatorin increased the intestinal absorption of puerarin and vincristine by inhibiting P-gp-mediated drug efflux. However; the underlying mechanism was not known. The present study investigated the mechanism by which imperatorin promotes P-gp-mediated drug transport. We used molecular docking to predict the binding force between imperatorin and P-gp and the effect of imperatorin on P-gp activity...
November 24, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27883364/determination-of-s-methyl-l-methionine-smm-from-brassicaceae-family-vegetables-and-characterization-of-the-intestinal-transport-of-smm-by-caco-2-cells
#8
Ji-Hoon Song, Hae-Rim Lee, Soon-Mi Shim
The objectives of the current study were to determine S-methyl-L-methionine (SMM) from various Brassicaceae family vegetables by using validated analytical method and to characterize the intestinal transport mechanism of SMM by the Caco-2 cells. The SMM is well known to provide therapeutic activity in peptic ulcers. The amount of SMM from various Brassicaceae family vegetables ranged from 89.08 ± 1.68 μg/g to 535.98 ± 4.85 μg/g of dry weight by using validated ultra-performance liquid chromatography-electrospray ionization-mass spectrometry method...
November 24, 2016: Journal of Food Science
https://www.readbyqxmd.com/read/27877046/comparative-effect-and-safety-of-verapamil-in-keloid-and-hypertrophic-scar-treatment-a-meta-analysis
#9
Zhouna Li, Zhehu Jin
BACKGROUND: Keloids and hypertrophic scars are the most common types of pathological scarring. Traditionally, keloids have been considered as a result of aberrant wound healing, involving excessive fibroblast participation that is characterized by hyalinized collagen bundles. However, the usefulness of this characterization has been questioned. In recent years, studies have reported the appropriate use of verapamil for keloids and hypertrophic scars. METHODS: Searches were conducted on the databases Medline, Embase, Cochrane, PubMed, and China National Knowledge Infrastructure from 2006 to July 2016...
2016: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/27876352/quantitative-analysis-of-pharmacokinetic-profiles-of-verapamil-and-drug-drug-interactions-induced-by-a-cyp-inhibitor-using-a-stable-isotope-labeled-compound
#10
Makoto Kataoka, Chie Kojima, Kazuki Ueda, Keiko Minami, Haruki Higashino, Shinji Sakuma, Kazutaka Togashi, Kuninori Mutaguchi, Shinji Yamashita
The purpose of the present study is to demonstrate a useful approach (isotope-IV method) for analyzing drug-drug interactions (DDIs) following the oral administration of drugs using stable isotope-labeled compounds. Verapamil hydrochloride (VER) was used as a drug model. Deuterium-labeled VER (VER-d6, 0.005 mg/kg) was intravenously administered to rats with or without a pre-treatment with 1-aminobenzotriazole (ABT, 100 mg/kg), a potent CYP inhibitor, 1.5 h after the oral administration of VER (1 mg/kg)...
August 18, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27863655/direct-in-vivo-evidence-on-the-mechanism-by-which-nanoparticles-facilitate-the-absorption-of-a-water-insoluble-p-gp-substrate
#11
Ramesh Soundararajan, Kenji Sasaki, Lisa Godfrey, Uchechukwu Odunze, Nancy Fereira, Andreas Schätzlein, Ijeoma Uchegbu
Here we examine the mechanisms by which nanoparticles enable the oral absorption of water-insoluble, P-glycoprotein efflux pump (P-gp) substrates, without recourse to P-gp inhibitors. Both 200nm paclitaxel N-(2-phenoxyacetyl)-6-O-glycolchitosan (GCPh) nanoparticles (GCPh-PTX) and a simulated Taxol formulation, facilitate drug dissolution in biorelevant media, unlike paclitaxel nanocrystals. Verapamil (40mgkg(-1)) increased the oral absorption from low dose Taxol (6 or 10mgkg(-1)) by 100%, whereas the oral absorption from high dose Taxol (20mgkg(-1)) or low dose GCPh-PTX (6 or 10mgkg(-1)) was largely unchanged by verapamil...
November 30, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27856310/l-type-calcium-channel-antagonism-translation-from-in-vitro-to-in-vivo
#12
Bernard Fermini, David S Ramirez, Sunny Sun, Asser Bassyouni, Michelle Hemkens, Todd Wisialowski, Stephen Jenkinson
INTRODUCTION: Although therapeutically beneficial in the treatment of certain diseases, L-type calcium channel antagonism can result in unwanted off-target pharmacology leading to adverse drug reactions and to the termination of the development of otherwise promising compounds. In the present study three marketed calcium channel inhibitors, nifedipine, verapamil and diltiazem were profiled in a series of in vitro and ex-vivo assays in an effort to determine the ability of these assays to discriminate, between dihydropyridine versus non-dihydropyridine-like compounds, and how well they can predict the cardiovascular effects observed in a conscious telemetered rat model...
November 15, 2016: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/27836711/effect-of-cigarette-smoke-extract-on-p-glycoprotein-function-in-primary-cultured-and-newly-developed-alveolar-epithelial-cells
#13
Mikihisa Takano, Ryosuke Naka, Yoshihiro Sasaki, Saori Nishimoto, Ryoko Yumoto
The effect of cigarette smoke extract (CSE) on P-glycoprotein (P-gp) function in the distal lung is unclear. In this study, we first examined the expression and function of P-gp and the effect of CSE in rat primary cultured alveolar epithelial cells. The expression of P-gp protein was observed in type I-like cells, but not in type II cells. In type I-like cells, rhodamine 123 (Rho123) accumulation was enhanced by various P-gp inhibitors such as verapamil and cyclosporine A. In addition, the expression of P-gp mRNAs, mdr1a and mdr1b, as well as P-gp activity increased along with the transdifferentiation...
August 31, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27814696/requirement-of-abc-transporter-inhibition-and-hoechst-33342-dye-deprivation-for-the-assessment-of-side-population-defined-c6-glioma-stem-cell-metabolism-using-fluorescent-probes
#14
Yoshitaka Murota, Kouichi Tabu, Tetsuya Taga
BACKGROUND: Elucidating the precise properties of cancer stem cells (CSCs) is indispensable for the development of effective therapies against tumors, because CSCs are key drivers of tumor development, metastasis and relapse. We previously reported that the Hoechst 33342 dye-low staining side population (SP) method can enrich for CSCs in the C6 glioma cell line, and that the positively stained main population (MP) cells are non-CSCs. Presence of cancer stem-like SP cells is reported in various types of cancer...
November 4, 2016: BMC Cancer
https://www.readbyqxmd.com/read/27813130/p-glycoprotein-inhibition-sensitizes-human-breast-cancer-cells-to-proteasome-inhibitors
#15
Rahul R Deshmukh, Seongho Kim, Yasmine Elghoul, Q Ping Dou
Although effective for the treatment of hematological malignancies, the FDA approved proteasome inhibitors bortezomib and carfilzomib have limited efficacy in solid tumors including triple negative breast cancer (TNBC). Chemotherapy is the only option for treating TNBC due to the absence of specific therapeutic targets. Therefore, development of new TNBC therapeutic strategies has been warranted. We studied whether P-glycoprotein (P-gp) inhibition could sensitize TNBC cells to proteasome inhibitors. When verapamil, a P-gp inhibitor, was combined with the proteasome inhibitor MG132, bortezomib or carfilzomib, the cytotoxic effects and apoptosis in TNBC MDA-MB-231 cells were enhanced, compared to each treatment alone...
November 4, 2016: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/27812957/the-effects-of-verapamil-and-its-combinations-with-glutamate-and-glycine-on-cardiodynamics-coronary-flow-and-oxidative-stress-in-isolated-rat-heart
#16
Isidora Stojic, Ivan Srejovic, Vladimir Zivkovic, Nevena Jeremic, Marko Djuric, Ana Stevanovic, Tamara Milanovic, Dragan Djuric, Vladimir Jakovljevic
The role of N-methyl-D-aspartate receptor (NMDA-R) in heart is still unclear. For these ionotropic glutamate receptors is characteristic the necessity of both co-agonists, glutamate and glycine, for their activation, which primarily allows influx of calcium. The aim of the present study was to examine the effects of verapamil, as a calcium channel blocker, alone and its combination with glycine and/or glutamate on cardiac function, coronary flow, and oxidative stress in isolated rat heart or to examine the effects of potential activation of NMDA-R in isolated rat heart...
November 3, 2016: Journal of Physiology and Biochemistry
https://www.readbyqxmd.com/read/27810590/structure-activity-relationship-study-of-novel-2-aminobenzofuran-derivatives-as-p-glycoprotein-inhibitors
#17
Chien-Yu Chen, Chin-Min Lin, Hui-Chang Lin, Chien-Fu Huang, Chih-Yu Lee, Tze-Chun Si Tou, Chin-Chuan Hung, Chih-Shiang Chang
Treatment of cancer patients with chemotherapeutic drugs is often associated with the occurrence of tumors with a multidrug resistance (MDR). Furthermore, the relation between overexpression of P-glycoprotein (P-gp) and resistant cancers has been well established. In this study, novel 2-aminobenzofuran derivatives were synthesized and tested for their ability to modulate P-gp mediated multidrug resistance (MDR) in vitro. The most potent compound, 43, increased P-gp inhibitory activity at 5 μM by 11.12-fold and was 3...
August 22, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27810576/effects-of-pharmaceuticals-and-personal-care-products-ppcps-on-multixenobiotic-resistance-mxr-related-efflux-transporter-activity-in-zebrafish-danio-rerio-embryos
#18
V Cunha, K Burkhardt-Medicke, P Wellner, M M Santos, P Moradas-Ferreira, T Luckenbach, M Ferreira
Certain ATP binding cassette (ABC) transporter proteins, such as zebrafish Abcb4, are efflux pumps acting as a cellular defence against a wide range of different, potentially toxic chemical compounds thus mediating so called multixenobiotic resistance (MXR). Certain chemicals target MXR proteins and, as so called chemosensitisers, inhibit the activity of these proteins thus increasing the toxicity of other chemicals that would normally be effluxed. In this study 14 pharmaceuticals and personal care products (PPCPs) that are being increasingly detected in aquatic systems, were assessed for interference with the MXR system of zebrafish (Danio rerio)...
October 28, 2016: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/27804872/prediction-and-early-evaluation-of-anticancer-therapy-response-from-imaging-of-drug-efflux-pumps-to-targeted-therapy-response
#19
Qingqing Menga, Zheng Lib, Shaoshun Li
Multidrug resistance (MDR) describes the resistance of tumor cells to chemotherapy and has been ascribed to the overexpression of drug efflux pumps. Molecular imaging of drug efflux pumps is helpful to identify the patients who may be resistant to the chemotherapy and thus will avoid the unnecessary treatment and increase the therapeutic effectiveness. Imaging probes targeting drug efflux pumps can non-invasively evaluate the Pgp function and play an important role in identification of MDR, prediction of response, and monitoring MDR modulation...
November 1, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27804305/spasmolytic-effect-of-jasonia-glutinosa-on-rodent-intestine
#20
Marta Castro, Mariano Ramón Giménez, Francisco Les Pereda, Lorena Trejo, Miguel Ángel Plaza, Víctor López, María Divina Murillo, Marta Sofia Valero Gracia
INTRODUCTION: Jasonia glutinosa is an endemic plant species of the Iberian Peninsula and Southern France traditionally used in infusions as a spasmolytic; this plant is also known as "té de roca" (rock tea) but there is no scientific evidence about the effects of this plant. AIM: To evaluate the spasmolytic effect of rock tea. METHODS: We have studied the in vitro effect of a rock tea extract on rat duodenum spontaneous contractions and the in vivo effect on mice gastrointestinal transit...
November 2, 2016: Revista Española de Enfermedades Digestivas
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