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https://www.readbyqxmd.com/read/28430559/heart-on-a-chip-an-investigation-of-the-influence-of-static-and-perfusion-conditions-on-cardiac-h9c2-cell-proliferation-morphology-and-alignment
#1
Anna Kobuszewska, Ewelina Tomecka, Kamil Zukowski, Elzbieta Jastrzebska, Michal Chudy, Artur Dybko, Philippe Renaud, Zbigniew Brzozka
Lab-on-a-chip systems are increasingly used as tools for cultures and investigation of cardiac cells. In this article, we present how the geometry of microsystems and microenvironmental conditions (static and perfusion) influence the proliferation, morphology, and alignment of cardiac cells (rat cardiomyoblasts-H9C2). Additionally, studies of cell growth after incubation with verapamil hydrochloride were performed. For this purpose, poly(dimethylsiloxane) (PDMS)/glass microfluidic systems with three different geometries of microchambers (a circular chamber, a longitudinal channel, and three parallel microchannels separated by two rows of micropillars) were prepared...
April 1, 2017: SLAS Technology
https://www.readbyqxmd.com/read/28429604/intra-arterial-verapamil-post-thrombectomy-is-feasible-safe-and-neuroprotective-in-stroke
#2
Justin F Fraser, Michael Maniskas, Amanda Trout, Doug Lukins, Lindsey Parker, W Lane Stafford, Abdulnasser Alhajeri, Jill Roberts, Gregory J Bix
Large vessel ischemic stroke represents the most disabling subtype. While t-PA and endovascular thrombectomy can recanalize the occluded vessel, good clinical outcomes are not uniformly achieved. We propose that supplementing endovascular thrombectomy with superselective intra-arterial (IA) verapamil immediately following recanalization could be safe and effective. Verapamil, a calcium channel blocker, has been shown to be an effective IA adjunct in a pre-clinical mouse focal ischemia model. To demonstrate translational efficacy, mechanism, feasibility, and safety, we conducted a group of translational experiments...
January 1, 2017: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/28427048/1-25-dihydroxyvitamin-d3-attenuates-the-effects-of-lipopolysaccharide-by-causing-adam10-dependent-ectodomain-shedding-of-toll-like-receptor-4
#3
Won Seok Yang, Jin Ju Kim, Nam Jeong Han, Eun Kyoung Lee, Su-Kil Park
BACKGROUND/AIMS: We investigated how 1,25-dihydroxyvitamin D3 (1,25D3) inhibits the effects of lipopolysaccharide (LPS) in human aortic endothelial cells. METHODS: Cellular signaling was explored by determination of protein abundance with Western blot, measurement of cytosolic Ca2+ concentration and immunofluorescence staining for a disintegrin and metalloprotease 10 (ADAM10). RESULTS: LPS stimulated the expression of intercellular adhesion molecule 1 (ICAM-1) through toll-like receptor 4 (TLR4) and subsequent activation of p38 mitogen-activated protein kinase (p38 MAPK)...
April 17, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28424793/a-model-based-meta-analysis-evaluating-gender-differences-on-blood-flow-responses-to-brachial-artery-infusions-of-acetylcholine-albuterol-atp-bradykinin-estradiol-glyceryl-trinitrate-l-nmma-nevibolol-norepinephrine-sodium-nitroprusside-substance-p-and-verapamil
#4
Andy R Eugene
INTRODUCTION: Numerous studies have emerged over the course of several decades describing the properties of drugs eliciting vasodilatory or vasoconstrictor responses in the human vasculature. During drug development, decisions to move forward with testing with a new chemical entity are very costly. To fund or not to fund development, go or no-go, decisions are often limited by efficacy comparisons with the current products on the market. The primary aim of this paper is to use dose-response modeling and simulations to quantify differences in blood flow to Acetylcholine, Albuterol, ATP, Bradykinin, 17β-Estradiol, Glyceryl Trinitrate, L-NMMA, Nevibolol, Norepinephrine, Sodium Nitroprusside, Substance P, and Verapamil...
June 2016: MEDtube Science
https://www.readbyqxmd.com/read/28423656/effect-of-y6-an-epigallocatechingallate-derivative-on-reversing-doxorubicin-drug-resistance-in-human-hepatocellular-carcinoma-cells
#5
Yan Wen, Rui-Qiang Zhao, Yun-Kai Zhang, Pranav Gupta, Li-Xiang Fu, An-Zhou Tang, Bu-Ming Liu, Zhe-Sheng Chen, Dong-Hua Yang, Gang Liang
Cancer cells can acquire resistance to a wide variety of diverse and unrelated drugs, this phenomenon is termed multidrug resistance (MDR). Multidrug resistance has been an obstacle to the success of cancer chemotherapy. The present study investigated the reversal effect of Y6, a new compound obtained by chemically modifying the structure of epigallocatechin-3-gallate (EGCG) extracted from green tea. Y6 was proven to be effective in inhibiting cell proliferation and reversing drug resistance in doxorubicin (DOX) resistant human hepatocellular carcinoma cells (BEL-7404/DOX)...
March 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28421447/inhibition-of-p-glycoprotein-stimulates-cell-death-under-hypoxia-mimicking-conditions
#6
A S Vdovin, P V Maximchik, A V Kulikov, B D Zhivotovsky, V G Gogvadze
The most common drug resistance mechanism in tumor cells is expression on their surface of the energy-dependent pump like P-glycoprotein (P-gp) that expels chemotherapeutic agents from the interior. An imitation of the hypoxic condition by the iron chelator deferoxamine caused Hypoxia-inducible factor 1-alpha (HIF-1α) stabilization and inhibition of doxorubicin-induced apoptosis in colon cancer НСТ116 cells. P-gp blocker verapamil suppressed doxorubicin accumulation leading to cell death induction. Considering these results, P-gp may be used as a potential target to stimulate chemotherapeutic drugs activity that will contribute to more efficient tumor cells elimination...
January 2017: Doklady. Biochemistry and Biophysics
https://www.readbyqxmd.com/read/28416541/efflux-attenuates-the-anti-bacterial-activity-of-q203-in-mycobacterium-tuberculosis
#7
Jichan Jang, Ryangyeo Kim, Minjeong Woo, Jinsun Jeong, Da Eun Park, Guehye Kim, Vincent Delorme
New and improved treatments for tuberculosis (TB) are urgently needed. Recently, it has been demonstrated that verapamil, an efflux inhibitor, can reduce bacterial drug tolerance caused by efflux pump activity when administered in combination with available anti-tuberculosis agents. The aim of this study was to evaluate the effectiveness of verapamil in combination with the anti-tuberculosis drug candidate Q203, which has recently been developed and is currently under clinical trials as a potential anti-tuberculosis agent...
April 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28401570/effect-of-p-glycoprotein-inhibition-at-the-blood-brain-barrier-on-brain-distribution-of-r-11-c-verapamil-in-elderly-versus-young-subjects
#8
Martin Bauer, Beatrix Wulkersdorfer, Rudolf Karch, Cécile Philippe, Walter Jäger, Johann Stanek, Wolfgang Wadsak, Marcus Hacker, Markus Zeitlinger, Oliver Langer
AIMS: The efflux transporter P-glycoprotein (ABCB1) restricts at the blood-brain barrier (BBB) distribution of many different drugs from blood to the brain. Previous data suggest an age-associated decrease in the expression and function of ABCB1 at the BBB. In this study we investigated the influence of age on the magnitude of an ABCB1-mediated drug-drug interaction (DDI) at the BBB. METHODS: We performed positron emission tomography (PET) scans with the model ABCB1 substrate (R)-[(11) C]verapamil in five young (26 ± 1 years, [mean ± standard deviation]) and five elderly (68 ± 6 years) healthy male volunteers before and after intravenous administration of a low dose of the ABCB1 inhibitor tariquidar (3 mg kg(-1) )...
April 12, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28400197/cutaneous-penetration-enhancing-effect-of-menthol-calcium-involvement
#9
Amit Joshi, Abhay Joshi, Hiren Patel, Dovenia Ponnoth, Grazia Stagni
Menthol is a naturally occurring terpene used as a penetration enhancer in topical and transdermal formulations. Literature shows a growing interest on menthol's interactions with the Transient-Receptor-Potential (TRPM-8) calcium channel. A decrease in extracellular Ca(+2) due to the activation of TRPM-8 channels produces inhibition of E-cadherin expression that is responsible for cell-cell adhesion. Since calcium is present in the entire epidermis, the purpose of this study is to evaluate whether the aforementioned properties of menthol are also related to its penetration-enhancing-effects...
April 8, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28393067/biophysical-and-pharmacological-characterization-of-energy-dependent-efflux-of-sb-in-laboratory-selected-resistant-strains-of-leishmania-viannia-subgenus
#10
Priscila G Dos Reis, Rubens L do Monte-Neto, Maria N Melo, Frédéric Frézard
The growing resistance of leishmaniasis to first-line drugs like antimonials in some regions limits the control of this parasitic disease. The precise mechanisms involved in Leishmania antimony resistance are still subject to debate. The reduction of intracellular Sb(III) accumulation is a common change observed in both laboratory-selected and field isolated resistant Leishmania strains, but the exact transport pathways involved in antimony resistance have not yet been elucidated. In order to functionally characterize the antimony transport routes responsible for resistance, we performed systematic transport studies of Sb(III) in wild-type and resistant strains of L...
2017: Frontiers in Cell and Developmental Biology
https://www.readbyqxmd.com/read/28389777/contribution-of-tumor-endothelial-cells-to-drug-resistance-anti-angiogenic-tyrosine-kinase-inhibitors-act-as-p-glycoprotein-antagonists
#11
MariaRosa Bani, Alessandra Decio, Raffaella Giavazzi, Carmen Ghilardi
Tumor endothelial cells (TEC) differ from the normal counterpart, in both gene expression and functionality. TEC may acquire drug resistance, a characteristic that is maintained in vitro. There is evidence that TEC are more resistant to chemotherapeutic drugs, substrates of ATP-binding cassette (ABC) transporters. TEC express p-glycoprotein (encoded by ABCB1), while no difference in other ABC transporters was revealed compared to normal endothelia. A class of tyrosine kinase inhibitors (TKI), used as angiostatic compounds, interferes with the ATPase activity of p-glycoprotein, thus impairing its functionality...
April 7, 2017: Angiogenesis
https://www.readbyqxmd.com/read/28386068/salvia-fruticosa-induces-vasorelaxation-in-rat-isolated-thoracic-aorta-role-of-the-pi3k-akt-enos-no-cgmp-signaling-pathway
#12
M Akhtar Anwar, Ali A Samaha, Samar Ballan, Alaaeldin I Saleh, Rabah Iratni, Ali H Eid
Salvia fruticosa (SF) Mill. is traditionally used for its antihypertensive actions. However, little is known about its pharmacologic and molecular mechanisms of action. Here we determined the effects of an ethanolic extract of SF leaves on rings of isolated thoracic aorta from Sprague-Dawley rats. Our results show that SF extract increased nitric oxide production and relaxed endothelium-intact rings in a dose-dependent (0.3 µg/ml-1 mg/ml) manner, and the maximum arterial relaxation (Rmax) was significantly reduced with endothelium denudation...
April 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28385544/a-prediction-method-for-p-glycoprotein-mediated-drug-drug-interactions-at-the-human-blood-brain-barrier-from-blood-concentration-time-profiles-validated-with-pet-data
#13
Akihiro Matsuda, Rudolf Karch, Martin Bauer, Alexander Traxl, Markus Zeitlinger, Oliver Langer
The purpose of this study was to establish physiologically based pharmacokinetic (PBPK) models to predict in humans the brain concentration-time profiles and P-glycoprotein (Pgp)-mediated brain drug-drug interactions (DDIs) between the model Pgp substrate (R)-[(11)C]verapamil (VPM), the model dual Pgp/breast cancer resistance protein (BCRP) substrate [(11)C]tariquidar (TQD) and the Pgp inhibitor tariquidar. The model predictions were validated with results from positron emission tomography (PET) studies in humans...
April 3, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28381797/development-of-cassette-pampa-for-permeability-screening
#14
Mun Hwan Oh, Hye Jin Lee, Sang Hyun Jo, Bernie Byunghoon Park, Sae-Bom Park, Eun-Yeong Kim, Yuanyuan Zhou, Young Ho Jeon, Kiho Lee
The parallel artificial membrane permeability assay (PAMPA) is widely used in early-stage drug discovery to discriminate compounds by intestinal permeability. The purpose of the current study was to establish a cassette (n-in-1) PAMPA to enable permeability screening of lipophilic compounds. A double-sink PAMPA consisting of a pH gradient (i.e., pH 6.5 and 7.4 for the donor and receiver compartments, respectively) and a lipophilic sink (i.e., a surfactant in the receiver solution) was utilized with cassette incubation of 10 reference compounds...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28381360/introduction-of-agarose-gel-as-a-green-membrane-in-electromembrane-extraction-an-efficient-procedure-for-the-extraction-of-basic-drugs-with-a-wide-range-of-polarities
#15
Hadi Tabani, Sakine Asadi, Saeed Nojavan, Mitra Parsa
Developing green methods for analyte extraction is one of the most important topics in the field of sample preparation. In this study, for the first time, agarose gel was used as membrane in electromembrane extraction (EME) without using any organic solvent, for the extraction of four model basic drugs (rivastigmine (RIV), verapamil (VER), amlodipine (AML), and morphine (MOR)) with a wide polarity window (log P from 0.43 to 3.7). Different variables playing vital roles in the proposed method were evaluated and optimized...
March 29, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28368479/verapamil-use-is-associated-with-reduction-of-newly-diagnosed-diabetes-mellitus
#16
Ti Yin, Shu-Chen Kuo, Yea-Yuan Chang, Yung-Tai Chen, Kai-Wei Katherine Wang
Objective: The mechanism of the beneficial effect of calcium channel blockers (CCBs), especially verapamil, on the development of type 2 diabetes mellitus (T2DM) has been described. Previous clinical studies aiming to confirm these results were flawed by inappropriate comparator drugs or study designs. This study compared the incidence of T2DM in adults prescribed oral verapamil and propensity score-matched adults prescribed other oral CCBs. Methods: This retrospective population-based cohort study used Taiwan's National Health Insurance Research Database during 2000-2011...
March 24, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28367925/selective-absorption-of-dietary-sphingoid-bases-from-the-intestine-via-efflux-by-p-glycoprotein-in-rats
#17
Aoi Fujii, Yuki Manabe, Kazuhiko Aida, Tsuyoshi Tsuduki, Takashi Hirata, Tatsuya Sugawara
Various physiological functions of dietary sphingolipids, such as preventing inflammation and improving the skin barrier function, have been recently demonstrated. The sphingolipid most commonly used as a foodstuff is glucosylceramide from plant sources, which is composed of sphingoid bases that are distinctive from those found in mammals. Although the structure of sphingoid bases in higher plants is more complicated than the structure of those in mammals, the fate of dietary sphingolipids of plant origin is still not understood...
2017: Journal of Nutritional Science and Vitaminology
https://www.readbyqxmd.com/read/28366566/chromatographic-studies-of-drug-interactions-with-alpha1-acid-glycoprotein-by-ultrafast-affinity-extraction-and-peak-profiling
#18
Sandya Beeram, Cong Bi, Xiwei Zheng, David S Hage
Interactions with serum proteins such as alpha1-acid glycoprotein (AGP) can have a significant effect on the behavior and pharmacokinetics of drugs. Ultrafast affinity extraction and peak profiling were used with AGP microcolumns to examine these processes for several model drugs (i.e., chlorpromazine, disopyramide, imipramine, lidocaine, propranolol and verapamil). The association equilibrium constants measured for these drugs with soluble AGP by ultrafast affinity extraction were in the general range of 10(4)-10(6)M(-1) at pH 7...
May 12, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28352965/dual-energy-ct-to-diagnose-pseudoedema-in-contrast-induced-encephalopathy-following-cerebral-angiography
#19
Gabriel L Pagani-Estévez, Deena M Nasr, Waleed Brinjikji, Avital Perry, Jennifer E Fugate
BACKGROUND: Contrast-induced encephalopathy (CIE) is a syndrome that may be clinically unrecognized and misdiagnosed as cerebral edema. METHODS: Case report and review. RESULTS: A 72-year-old woman was admitted for elective endovascular embolization of a 10-mm left anterior communicating artery aneurysm. One hour post-procedure, she acutely developed global aphasia. Emergent head computed tomography (CT) and computed tomography-angiography (CTA) showed high attenuation of the left hemispheric subarachnoid spaces interpreted as hemispheric edema; emergent magnetic resonance imaging revealed left hemispheric punctate infarcts...
March 28, 2017: Neurocritical Care
https://www.readbyqxmd.com/read/28351325/intracellular-calcium-promotes-radioresistance-of-non-small-cell-lung-cancer-a549-cells-through-activating-akt-signaling
#20
Yiling Wang, Jiantao He, Shenghui Zhang, Qingbo Yang
Radiotherapy is a major therapeutic approach in non-small cell lung cancer but is restricted by radioresistance. Although Akt signaling promotes radioresistance in non-small cell lung cancer, it is not well understood how Akt signaling is activated. Since intracellular calcium (Ca(2+)) could activate Akt in A549 cells, we investigated the relationship between intracellular calcium (Ca(2+)) and Akt signaling in radioresistant A549 cells by establishing radioresistant non-small cell lung cancer A549 cells. The radioresistant cell line A549 was generated by dose-gradient irradiation of the parental A549 cells...
March 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
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