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https://www.readbyqxmd.com/read/28445860/brephedrone-a-new-psychoactive-substance-seized-in-brazil
#1
Yuri Machado, José Coelho Neto, Paulo Eduardo Nunes Barbosa, Rogério Araújo Lordeiro, Rosemeire Brondi Alves
At the beginning of 2015, sixty-two capsules containing red-brown crystals seized in a historical city in Brazil were sent to this forensic laboratory for drug testing analysis. The material was identified as being Brephedrone, a new psychoactive substance and a bromine synthetic cathinone that is related to serotonin transportation. This substance was analyzed by ATR-FTIR, GC-MS, LC-MS, (1)H, (13)C and 2D NMR. Brephedrone apprehensions have been previously reported in Finland, France and Spain. It was the first detection of this substance in the State of Minas Gerais...
April 15, 2017: Forensic Science International
https://www.readbyqxmd.com/read/28445595/ventricular-fibrillation-cardiac-arrest-produces-a-chronic-striatal-hyperdopaminergic-state-that-is-worsened-by-methylphenidate-treatment
#2
Gerald J Nora, Rashed Harun, David F Fine, Daniel Hutchison, Adam C Grobart, Jason P Stezoski, Miranda Munoz, Patrick M Kochanek, Rehana K Leak, Tomas Drabek, Amy K Wagner
Cardiac arrest survival rates have improved with modern resuscitation techniques, but many survivors experience impairments associated with hypoxic-ischemic brain injury. Currently, little is understood about chronic changes in striatal dopamine (DA) systems after hypoxic-ischemic brain injury. Given the common empiric clinical use of DA enhancing agents in neurorehabilitation, investigation evaluating dopaminergic alterations after cardiac arrest (CA) is necessary to optimize rehabilitation approaches. We hypothesized that striatal DA neurotransmission would be altered chronically after ventricular fibrillation cardiac arrest (VF-CA)...
April 26, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28445501/out-of-hospital-cardiac-arrest-survival-in-drug-related-versus-cardiac-causes-in-ontario-a-retrospective-cohort-study
#3
Aaron M Orkin, Chun Zhan, Jason E Buick, Ian R Drennan, Michelle Klaiman, Pamela Leece, Laurie J Morrison
BACKGROUND: Drug overdose causes approximately 183,000 deaths worldwide annually and 50,000 deaths in Canada and the United States combined. Drug-related deaths are concentrated among young people, leading to a substantial burden of disease and loss of potential life years. Understanding the epidemiology, patterns of care, and prognosis of drug-related prehospital emergencies may lead to improved outcomes. METHODS: We conducted a retrospective cohort study of out-of-hospital cardiac arrests with drug-related and presumed cardiac causes between 2007 and 2013 using the Toronto Regional RescuNet Epistry database...
2017: PloS One
https://www.readbyqxmd.com/read/28445053/sulfotransferases-and-breast-cancer-resistance-protein-determine-the-disposition-of-calycosin-in-vitro-and-in-vivo
#4
Jia Yu, Lijun Zhu, Haihui Zheng, Xia Gong, Jianghuang Yu, Jiamei Chen, Yuhuan Li, Hongming Zheng, Xiaoxiao Qi, Ying Wang, Ming Hu, Linlin Lu, Zhong Qiu Liu
Sulfation is a key process of drugs disposition that generally regulates the drug effectiveness and toxicity. Calycosin derived from the dry root extract of Radix Astragali exhibits a variety of biological effects that easily undergo extensive phase II metabolism. However, the sulfation pathway of calycosin lacks information. We investigated the disposition mechanisms of calycosin sulfate in vitro and in vivo. We characterized the sulfation metabolism and excretion of calycosin using bi-directional transport studies...
April 26, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28444472/the-effect-of-sodium-glucose-co-transporter-2-sglt-2-inhibitors-on-cardiometabolic-profile-beyond-the-hypoglycaemic-action
#5
Eirini Lioudaki, Emmanouil S Androulakis, Martin Whyte, Konstantinos G Stylianou, Eugenios K Daphnis, Emmanouil S Ganotakis
Type 2 diabetes mellitus (T2DM) has growing prevalence worldwide and major clinical implications, chiefly cardiovascular (CV) and renal disease burden. Sodium-glucose co-transporter (SGLT)-2 inhibitors are a new drug class in the management of T2DM with a mechanism of action independent of insulin. In addition to their hypoglycaemic effect, SGLT-2 inhibitors appear to have haemodynamic and nephroprotective effects. Studies have consistently showed a modest but significant blood pressure (BP) reduction. Metabolic benefits are also attributed to SGLT-2 inhibitors with a modest but consistent body weight decrease recorded along with improvements in lipid profile and uric acid levels...
April 25, 2017: Cardiovascular Drugs and Therapy
https://www.readbyqxmd.com/read/28444310/arl3-and-rp2-regulate-the-trafficking-of-ciliary-tip-kinesins
#6
Nele Schwarz, Amelia Lane, Katarina Jovanovich, David A Parfitt, Monica Aguila, Clare L Thompson, Lyndon da Cruz, Peter J Coffey, J Paul Chapple, Alison J Hardcastle, Michael E Cheetham
Ciliary trafficking defects are the underlying cause of many ciliopathies, including Retinitis Pigmentosa (RP). Anterograde intraflagellar transport (IFT) is mediated by kinesin motor proteins; however, the function of the homodimeric Kif17 motor in cilia is poorly understood, whereas Kif7 is known to play an important role in stabilising cilia tips. Here we identified the ciliary tip kinesins Kif7 and Kif17 as novel interaction partners of the small GTPase Arl3 and its regulatory GTPase activating protein (GAP) Retinitis Pigmentosa 2 (RP2)...
April 21, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28443362/effect-of-the-side-chain-spacer-structure-on-the-ph-responsive-properties-of-polycarboxylates
#7
Atsushi Harada, Ryoma Teranishi, Eiji Yuba, Kenji Kono
The properties of stimuli-responsive polymers change significantly with changes to their environment, such as temperature and pH. This behavior can be utilized for the preparation of stimuli-responsive carriers for efficient cytosolic delivery of active drugs. Among the possible environmental conditions, pH is one of the most useful stimuli because the pH in an endosome is lower than under physiological conditions, depending on endosomal development. This pH difference is an important factor in the design of pH-responsive polymers, which can be used to enhance the transport of endocytosed drugs from the endosomal compartment to the cytoplasm...
April 26, 2017: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/28443323/prevalence-of-ctr1-and-ercc1-polymorphisms-and-response-of-biliary-tract-cancer-to-gemcitabine-platinum-chemotherapy
#8
Skolchart Pongmaneratanakul, Suebpong Tanasanvimon, Thitima Pengsuparp, Nutthada Areepium
Purpose: Biliary tract cancer (BTC)is an aggressive disease with a poor prognosis. Most patients are diagnosed at an advanced stage for which curative surgery is not possible and gemcitabine-platinum chemotherapy is the treatment of choice for advanced cases. Several studies had focused on biomarkers to predict response from platinum drugs in lung cancer, but information is limited for BTC. In this study, two single nucleotide polymorphisms (SNPs) in the copper transporter (CTR1) and excision repair cross-complementary group 1 (ERCC1) genes were investigated as predictive biomarkers of objective response to gemcitabine-platinum...
March 1, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/28443244/the-mitochondrial-voltage-dependent-anion-channel-1-ca-2-transport-apoptosis-and-their-regulation
#9
REVIEW
Varda Shoshan-Barmatz, Soumasree De, Alon Meir
In the outer mitochondrial membrane, the voltage-dependent anion channel 1 (VDAC1) functions in cellular Ca(2+) homeostasis by mediating the transport of Ca(2+) in and out of mitochondria. VDAC1 is highly Ca(2+)-permeable and modulates Ca(2+) access to the mitochondrial intermembrane space. Intramitochondrial Ca(2+) controls energy metabolism by enhancing the rate of NADH production via modulating critical enzymes in the tricarboxylic acid cycle and fatty acid oxidation. Mitochondrial [Ca(2+)] is regarded as an important determinant of cell sensitivity to apoptotic stimuli and was proposed to act as a "priming signal," sensitizing the organelle and promoting the release of pro-apoptotic proteins...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/28442581/sigma-receptor-effects-of-n-substituted-benztropine-analogs-implications-for-antagonism-of-cocaine-self-administration
#10
Takato Hiranita, Weimin C Hong, Theresa Kopajtic, Jonathan L Katz
Several N-substituted benztropine (BZT) analogs are atypical dopamine transport inhibitors as they have affinity for the dopamine transporter (DAT), but have minimal cocaine-like pharmacological effects and can block numerous effects of cocaine including its self-administration. Among these compounds, N-methyl (AHN1-055), N-allyl (AHN2-005), and N-butyl (JHW007) analogs of 3α-[bis(4'-fluorophenyl)methoxy]-tropane were more potent in antagonizing self-administration of cocaine and d-methamphetamine than in decreasing food-maintained responding...
April 25, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28442499/absorption-distribution-metabolism-and-excretion-of-the-oral-prostaglandin-d2-receptor-2-dp2-antagonist-fevipiprant-qaw039-in-healthy-volunteers-and-in-vitro
#11
David Pearson, H Markus Weiss, Yi Jin, Jan Jaap van Lier, Veit J Erpenbeck, Ulrike Glaenzel, Peter End, Ralph Woessner, Fabian Eggimann, Gian Camenisch
Fevipiprant is a novel oral prostaglandin D2 receptor 2 (DP2; also known as CRTh2) antagonist, which is currently in development for the treatment of severe asthma and atopic dermatitis. We investigated the absorption, distribution, metabolism, and excretion properties of fevipiprant in healthy subjects after a single 200 mg oral dose of [(14)C]-radiolabeled fevipiprant. Fevipiprant and metabolites were analyzed by liquid chromatography coupled to tandem mass spectrometry and radioactivity measurements, and mechanistic in vitro studies were performed to investigate clearance pathways and covalent plasma protein binding...
April 25, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28441873/identification-and-characterization-of-a-secondary-sodium-binding-site-and-the-main-selectivity-determinants-in-the-human-concentrative-nucleoside-transporter-3
#12
C Arimany-Nardi, A Claudio-Montero, A Viel-Oliva, P Schmidtke, C Estarellas, X Barril, A Bidon-Chanal, M Pastor-Anglada
The family of concentrative Na(+):nucleoside cotransporters in humans is constituted by three subtypes, namely hCNT1, hCNT2 and hCNT3. Besides their different nucleoside selectivity, hCNT1 and hCNT2 have a Na(+):nucleoside stoichiometry of 1:1, while for hCNT3 it is of 2:1. This distinct stoichiometry of subtype 3 might hint the existence of a secondary sodium-binding site that is not present in the other two subtypes, but to date their three-dimensional structures remain unknown and the residues implicated in Na(+) binding are unclear...
April 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28441502/differential-coupling-of-binding-atp-hydrolysis-and-transport-of-fluorescent-probes-with-p-glycoprotein-in-lipid-nanodiscs
#13
Mavis Jiarong Li, Abhinav Nath, William M Atkins
The ATP-binding cassette transporter P-glycoprotein (ABCB1) plays a major role in cellular resistance to drugs, and drug interactions. Experimental studies support a mechanism with nucleotide-dependent fluctuation between inward-facing and outward-facing conformations, which are coupled to nucleotide hydrolysis. However, detailed insight into drug-dependent modulation of these conformational ensembles is lacking. Different drugs likely occupy partially overlapping but distinct sites, and are therefore variably coupled to nucleotide binding and hydrolysis...
April 25, 2017: Biochemistry
https://www.readbyqxmd.com/read/28441400/a-genomics-approach-identifies-selective-effects-of-trans-resveratrol-in-cerebral-cortex-neuron-and-glia-gene-expression
#14
Gemma Navarro, Eva Martínez-Pinilla, Alejandro Sánchez-Melgar, Raquel Ortiz, Véronique Noé, Mairena Martín, Carlos Ciudad, Rafael Franco
The mode of action of trans-resveratrol, a promising lead compound for the development of neuroprotective drugs, is unknown. Data from a functional genomics study were retrieved with the aim to find differentially expressed genes that may be involved in the benefits provided by trans-resveratrol. Genes that showed a significantly different expression (p<0.05, cut-off of a two-fold change) in mice fed with a control diet or a control diet containing trans-resveratrol were different in cortex, heart and skeletal muscle...
2017: PloS One
https://www.readbyqxmd.com/read/28440467/structural-and-evolutionary-divergence-of-aquaporins-in-parasites-review
#15
Zi-Xin Ni, Jian-Min Cui, Nian-Zhang Zhang, Bao-Quan Fu
Aquaporins are ubiquitous proteins that belong to the major intrinsic protein family. Previous studies have indicated that aquaporins are involved in multiple physiological processes in parasites, such as nutrient absorption and end product efflux, and thus, would be promising pharmacological agents in the fight against parasite infection. In the present paper, the authors analyzed the evolutionary relationship of parasitic aquaporins by re‑constructing of a phylogenic tree using neighbor‑joining and maximum likelihood methods...
April 25, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28440421/allicin-induces-the-upregulation-of-abca1-expression-via-ppar%C3%AE-lxr%C3%AE-signaling-in-thp-1-macrophage-derived-foam-cells
#16
Xiao-Long Lin, Hui-Jun Hu, Yuan-Bo Liu, Xue-Mei Hu, Xiao-Juan Fan, Wei-Wen Zou, Yong-Quan Pan, Wen-Quan Zhou, Min-Wen Peng, Cai-Hong Gu
Allicin is considered anti-atherosclerotic due to its antioxidant and anti-inflammatory effects, which makes it an important drug for the prevention and treatment of atherosclerosis. However, the effects of allicin on foam cells are unclear. Thus, in this study, we examined the effects of allicin on lipid accumulation via peroxisome proliferator-activated receptor γ (PPARγ)/liver X receptor α (LXRα) in THP‑1 macrophage-derived foam cells. THP‑1 cells were exposed to 100 nM phorbol myristate acetate (PMA) for 24 h, and then to oxydized low-density lipoprotein (ox-LDL; 50 mg/ml) to induce foam cell formation...
April 11, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28440199/anti-hyperglycemic-agents-for-the-treatment-of-type-2-diabetes-mellitus-role-in-cardioprotection-during-the-last-decade
#17
Duygu Kocyigit, Kadri Murat Gurses, Muhammed Ulvi Yalcin, Lale Tokgozoglu
Type 2 diabetic patients are known to have a tendency to develop cardiovascular (CV) disease (CVD), and related unfavourable outcomes such as heart failure, myocardial infarction (MI), cerebrovascular events (eg. stroke), and related mortality. Long- term clinical trials have revealed contradictory findings regarding the relationship between glycemic control and CV benefits due to variations in the key characteristics of the study population. During the last decade, number of pharmacological agents used for glucose- lowering in the treatment of type 2 diabetes mellitus (T2DM) has increased owing to the introduction of dipeptidyl peptidase- IV (DPP- IV) inhibitors, glucagon- like peptide- 1 (GLP- 1) receptor agonists, and sodium-glucose co-transporter 2 (SGLT- 2) inhibitors...
April 23, 2017: Endocrine, Metabolic & Immune Disorders Drug Targets
https://www.readbyqxmd.com/read/28439502/ambroxol-hydrochloride-combined-with-fluconazole-reverses-the-resistance-of-candida-albicans-to-fluconazole
#18
Xiuyun Li, Yuanhao Zhao, Xin Huang, Cuixiang Yu, Yilei Yang, Shujuan Sun
In this study, we found that ambroxol hydrochloride (128 μg/mL) exhibits synergistic antifungal effects in combination with fluconazole (2 μg/mL) against resistant planktonic Candida albicans (C. albicans) cells. This combination also exhibited synergistic effects against resistant C. albicans biofilms in different stages (4, 8, and 12 h) according to the microdilution method. In vitro data were further confirmed by the success of this combination in treating Galleria mellonella infected by resistant C. albicans...
2017: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/28438781/transporter-mediated-disposition-clinical-pharmacokinetics-and-cholestatic-potential-of-glyburide-and-its-primary-active-metabolites
#19
Rui Li, Yi-An Bi, Anna Vildhede, Renato J Scialis, Sumathy Mathialagan, Xin Yang, Lisa D Marroquin, Jian Lin, Manthena V S Varma
Glyburide is widely used for the treatment of type 2 diabetes mellitus. We studied the mechanisms involved in the disposition of glyburide and its pharmacologically active hydroxy metabolites, M1 and M2b; and evaluated their clinical pharmacokinetics and the potential role in glyburide-induced cholestasis employing physiologically based pharmacokinetic (PBPK) modeling. Transport studies of parent and metabolites in human hepatocytes and transfected cell systems imply hepatic uptake mediated by organic anion transporting polypeptides...
April 24, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28438535/a-critical-view-on-in-vitro-analysis-of-p-glycoprotein-p-gp-transport-kinetics
#20
Lasse Saaby, Birger Brodin
Transport proteins expressed in the different barriers of the human body can have great implications on absorption, distribution and excretion of drug compounds. Inhibition or saturation of a transporter can potentially alter these ADME properties, and thereby also the pharmacokinetic profile and bioavailability of drug compounds. P-glycoprotein (P-gp, ABCB1), is an efflux transporter which is present in most of the barriers of the body, including the small intestine, the blood-brain barrier, the liver and the kidney...
April 21, 2017: Journal of Pharmaceutical Sciences
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