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https://www.readbyqxmd.com/read/28231635/in-vivo-structural-imaging-in-rats-reveals-neuroanatomical-correlates-of-behavioral-sub-dimensions-of-cocaine-addiction
#1
Nazzareno Cannella, Alejandro Cosa-Linan, Elena Büchler, Claudia Falfan-Melgoza, Wolfgang Weber-Fahr, Rainer Spanagel
Cocaine addiction is a multi-dimensional behavioral disorder characterized by a loss of control over cocaine taking despite of detrimental consequences. Structural MRI studies have revealed association between cocaine consumption and gray matter volume (GMV) in cocaine-addicted patients. However, the behavioral correlates of GMV in cocaine addiction are poorly understood. Here, we used a DSM-IV-based rat model of cocaine addiction with high face validity for structural imaging. According to three behavioral sub-dimensions of addiction, rats were separated into two groups showing either addict-like or non-addict-like behavior...
February 23, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28231523/synergistic-effects-between-a-copper-based-metal-casiope%C3%A3-na-iii-ia-and-cisplatin
#2
Silvia Graciela Davila-Manzanilla, Yeshenia Figueroa-de-Paz, Carmen Mejia, Lena Ruiz-Azuara
Additive, subadditive or superadditive interactions observed in combination therapy play an important role in several treatments, particularly for cancer. The isobolographic analysis allows to establish the pharmacological interactions that exist between two drugs that are administered together in equieffective doses. In order to identify if the combination of two compounds presents synergistic interaction, the antiproliferative activity of CasIII-ia with analogue compounds or cisplatin in different molar ratios was evaluated...
February 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28231454/zinc-complexes-of-diflunisal-synthesis-characterization-structure-antioxidant-activity-and-in-vitro-and-in-silico-study-of-the-interaction-with-dna-and-albumins
#3
Alketa Tarushi, Chrisoula Kakoulidou, Catherine P Raptopoulou, Vassilis Psycharis, Dimitris P Kessissoglou, Ioanna Zoi, Athanasios N Papadopoulos, George Psomas
From the reaction of ZnCl2 with the non-steroidal anti-inflammatory drug diflunisal (Hdifl), complex [Zn(difl-O)2(MeOH)4], 1 was formed, while in the presence of a N,N'-donor heterocyclic ligand 2,2'-bipyridylamine (bipyam), 2,2'-bipyridine (bipy), 1,10-phenanthroline (phen) and 2,2'-dipyridylketone oxime (Hpko), the complexes [Zn(difl-O,O')2(bipyam)], 2, [Zn(difl-O,O')2(bipy)], 3, [Zn(difl-O,O')2(phen)], 4 and [Zn(difl-O)2(Hpko)2], 5 were isolated, respectively. The complexes were characterized by physicochemical and spectroscopic techniques and the crystal structures of complexes 2, 3 and 5 were determined by X-ray crystallography...
February 12, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28231453/siderophore-transport-by-mmpl5-mmps5-protein-complex-in-mycobacterium-tuberculosis
#4
Padmani Sandhu, Yusuf Akhter
Iron is an essential metal ion required for the various physiological activities of bacteria. The pathogenic bacteria remain dependent on the host cell for their iron requirements and evolved with specialized scavenging machinery in the form of iron chelating siderophores. Mycobacterium tuberculosis has two types of siderophore molecules, mycobactin and carboxymycobactin. These are synthesized inside bacterial cells and need to be transported outside by specialized membrane associated proteins. MmpL5-MmpS5 (mycobacterial membrane protein large5-mycobacterial membrane protein small5) complex has been linked to the export of non-ferrated siderophores to extracellular environment but the precise molecular mechanism involved was largely unknown...
February 14, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28231276/alterations-in-cellular-pharmacokinetics-and-pharmacodynamics-of-elvitegravir-in-response-to-ethanol-exposure-in-hiv-1-infected-monocytic-u1-cells
#5
Narasimha M Midde, Namita Sinha, Pradeep B Lukka, Bernd Meibohm, Santosh Kumar
Ethanol consumption is negatively associated with antiretroviral therapy (ART) adherence and general health in HIV positive individuals. Previously, we demonstrated ethanol-mediated alterations to metabolism of elvitegravir (EVG) in human liver microsomes. In the current study, we investigated ethanol influence on the pharmacokinetic and pharmacodynamic interactions of EVG in HIV infected monocytic (U1) cells. U1 cells were treated with 5 μM EVG, 2 μM Cobicistat (COBI), a booster drug, and 20 mM ethanol for up to 24 hours...
2017: PloS One
https://www.readbyqxmd.com/read/28231045/original-research-paper-public-health-care-system-a-quasi-experimental-study-acceptance-and-attitude-to-implicate-clinical-services
#6
Syed Wasif Gillani, Mohi Iqbal Mohammad Abdul
A six-month longitudinal intervention arm study with a pre-post cross-sectional questionnaire-based survey was performed. A 3-phase objective structured clinical examination (OSCE) design was utilized for evaluation of acceptance and attitude of pharmacy students towards clinical pharmacy services. The pre-OSCE survey showed increased disagreement with the role of clinical pharmacists, compared to a significant positive shift in attitude towards their services in the healthcare team after 6 months of the trial...
March 1, 2017: Acta Pharmaceutica
https://www.readbyqxmd.com/read/28231007/molecular-dynamics-recrystallization-behavior-and-water-solubility-of-amorphous-anticancer-agent-bicalutamide-and-its-polyvinylpyrrolidone-mixtures
#7
Justyna Szczurek, Marzena Rams-Baron, Justyna Knapik-Kowalczuk, Agata Antosik, Joanna Szafraniec, Witold Jamroz, Mateusz Dulski, Renata Jachowicz, Marian Paluch
In this paper, we investigated the molecular mobility and physical stability of amorphous bicalutamide, a poorly water-soluble drug widely used in prostate cancer treatment. Our broadband dielectric spectroscopy measurements and differential scanning calorimetry studies revealed that amorphous BIC is a moderately fragile material with strong tendency to recrystallize from amorphous state. However, mixing the drug with polymer polyvinylpyrrolidone results in a substantial improvement of physical stability attributed to antiplasticizing effect governing by polymer additive...
February 23, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28230985/discovery-of-competitive-and-non-competitive-ligands-of-the-organic-cation-transporter-1-oct1-slc22a1
#8
Eugene C Chen, Natalia Khuri, Xiaomin Liang, Adrian Stecula, Huan-Chieh Chien, Sook Wah Yee, Yong Huang, Andrej Sali, Kathleen M Giacomini
Organic cation transporter 1 (OCT1) plays a critical role in the hepatocellular uptake of structurally diverse endogenous compounds and xenobiotics. Here, we identified competitive and noncompetitive OCT1 interacting ligands in a library of 1,780 prescription drugs by combining in silico and in vitro methods. Ligands were predicted by docking against a comparative model based a eukaryotic homolog. In parallel, high-throughput screening (HTS) was conducted using the fluorescent probe substrate ASP+ in cells overexpressing human OCT1...
February 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28230564/attention-deficit-hyperactivity-disorder-aggression-and-illicit-stimulant-use-is-this-self-medication
#9
Annie P Odell, Grace L Reynolds, Dennis G Fisher, Loucine M Huckabay, William C Pedersen, Pamela Xandre, Milica Miočević
This study compares adults with and without attention deficit hyperactivity disorder (ADHD) on measures of direct and displaced aggression and illicit drug use. Three hundred ninety-six adults were administered the Wender Utah Rating Scale, the Risk Behavior Assessment, the Aggression Questionnaire (AQ), and the Displaced Aggression Questionnaire (DAQ). Those with ADHD were higher on all scales of the AQ and DAQ, were younger at first use of amphetamines, and were more likely to have ever used crack and amphetamines...
February 22, 2017: Journal of Nervous and Mental Disease
https://www.readbyqxmd.com/read/28230072/improved-social-interaction-recognition-and-working-memory-with-cannabidiol-treatment-in-a-prenatal-infection-poly-i-c-rat-model
#10
Ashleigh L Osborne, Nadia Solowij, Ilijana Babic, Xu-Feng Huang, Katrina Weston-Green
Neuropsychiatric disorders such as schizophrenia are associated with cognitive impairment, including learning, memory and attention deficits. Antipsychotic drugs are limited in their efficacy to improve cognition; therefore, new therapeutic agents are required. Cannabidiol (CBD), the non-intoxicating component of cannabis, has anti-inflammatory, neuroprotective and antipsychotic-like properties, however, its ability to improve the cognitive deficits of schizophrenia remains unclear. Using a prenatal infection model, we examined the effect of chronic CBD treatment on cognition and social interaction...
February 23, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28229955/three-dimensional-colloidal-lithography
#11
Hironori Nagai, Austen Poteet, Xu A Zhang, Chih-Hao Chang
Light interactions with colloidal particles can generate a variety of complex three-dimensional (3D) intensity patterns, which can be utilized for nanolithography. The study of particle-light interactions can add more types of intensity patterns by manipulating key factors. Here we investigate a novel 3D nanolithography technique using colloidal particles under two-beam coherent illuminations. The fabricated 3D nanostructures are hollow, nested within periodic structures, and possess multiple chamber geometry...
March 24, 2017: Nanotechnology
https://www.readbyqxmd.com/read/28229517/affinity-capillary-electrophoresis-and-fluorescence-spectroscopy-for-studying-enantioselective-interactions-between-omeprazole-enantiomer-and-human-serum-albumin
#12
Yujing Xu, Tingting Hong, Xueping Chen, Yibing Ji
Baseline separation of omeprazole (OME) enantiomers was achieved by affinity capillary electrophoresis (ACE), using human serum albumin (HSA) as the chiral selector. The influence of several experimental variables such as HSA concentration, the type and content of organic modifiers, applied voltage and running buffer concentration on the separation was evaluated. The binding of esomeprazole (S-omeprazole, S-OME) and its R-enantiomer (R-omeprazole, R-OME) to HSA under simulated physiological conditions was studied by ACE and fluorescence spectroscopy which was considered as a reference method...
February 23, 2017: Electrophoresis
https://www.readbyqxmd.com/read/28229443/-desvenlafaxine-and-neuropathic-pain-additional-clinical-benefits-of-a-second-generation-serotonin-noradrenaline-reuptake-inhibitor
#13
REVIEW
A Alcantara-Montero
INTRODUCTION: Desvenlafaxine is the third antidepressant within the group of serotonin-norepinephrine reuptake inhibitors. The latest clinical practice guidelines consulted agree that tricyclic antidepressants, dual (venlafaxine/duloxetine) and gabapentin/pregabalin antiepileptics, are the first-line drugs in the treatment of neuropathic pain, being tramadol, lidocaine 5% patches and capsaicin 8% patches of second-line drugs, while strong opioids constitute a third line treatment. The interaction between the binomial pain and depression is very frequent, being the psychological complication more frequent in patients with chronic pain...
March 1, 2017: Revista de Neurologia
https://www.readbyqxmd.com/read/28229376/the-pharmacogenetics-of-tacrolimus-in-corticosteroid-sparse-pediatric-and-adult-kidney-transplant-recipients
#14
Mads Juul Madsen, Troels K Bergmann, Kim Brøsen, Helle Charlotte Thiesson
INTRODUCTION: Tacrolimus is a calcineurin inhibitor used as an immunosuppressant drug in solid organ transplantation, and is mainly metabolized by cytochrome P450 (CYP) 3A4 and CYP3A5. Studies have shown an association between the CYP3A5 genotype and tacrolimus dose-adjusted trough concentrations. Variants in the genes PPARA, POR and CYP3A4 have recently been shown to influence tacrolimus metabolism. Furthermore, pharmacokinetic interaction between corticosteroid treatment and tacrolimus has been shown...
February 22, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28229375/clinical-pharmacokinetics-of-ombitasvir
#15
REVIEW
Prajakta S Badri, Diana L Shuster, Sandeep Dutta, Rajeev M Menon
Ombitasvir is a potent, nonstructural protein 5A inhibitor of the hepatitis C virus (HCV) that is used in combination with other direct-acting antivirals for the treatment of chronic HCV infection. Ombitasvir is predominantly metabolized by amide hydrolysis followed by oxidative metabolism and is a substrate of P-glycoprotein. Ombitasvir displays linear pharmacokinetics with minimal accumulation and is eliminated via metabolism and biliary excretion. A negligible amount of unchanged drug is excreted in urine...
February 22, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28229140/partitioning-of-caffeine-in-lipid-bilayers-reduces-membrane-fluidity-and-increases-membrane-thickness
#16
Adree Khondker, Alexander Dhaliwal, Richard J Alsop, Jennifer Tang, Matilda Backholm, An-Chang Shi, Maikel C Rheinstädter
Caffeine is a small amphiphilic molecule, which is widely consumed as a stimulant to prevent fatigue, but is also used as a common drug adjuvant in modern medicine. Here, we show that caffeine interacts with unsaturated lipid membranes made of 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC). By combining X-ray diffraction and molecular dynamics simulations, we present evidence that caffeine partitions in lipid membranes and locates at the head group-tail group interface of the bilayers. By attracting water molecules from neighboring lipid molecules, it leads to the formation of "water pockets", i...
February 23, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28228927/computational-approaches-for-revealing-the-structure-of-membrane-transporters-case-study-on-bilitranslocase
#17
REVIEW
Katja Venko, A Roy Choudhury, Marjana Novič
The structural and functional details of transmembrane proteins are vastly underexplored, mostly due to experimental difficulties regarding their solubility and stability. Currently, the majority of transmembrane protein structures are still unknown and this present a huge experimental and computational challenge. Nowadays, thanks to X-ray crystallography or NMR spectroscopy over 3000 structures of membrane proteins have been solved, among them only a few hundred unique ones. Due to the vast biological and pharmaceutical interest in the elucidation of the structure and the functional mechanisms of transmembrane proteins, several computational methods have been developed to overcome the experimental gap...
2017: Computational and Structural Biotechnology Journal
https://www.readbyqxmd.com/read/28228859/dynamics-and-interactions-of-ibuprofen-in-cyclodextrin-nanosponges-by-solid-state-nmr-spectroscopy
#18
Monica Ferro, Franca Castiglione, Nadia Pastori, Carlo Punta, Lucio Melone, Walter Panzeri, Barbara Rossi, Francesco Trotta, Andrea Mele
Two different formulations of cyclodextrin nanosponges (CDNS), obtained by polycondensation of β-cyclodextrin with ethylenediaminetetraacetic acid dianhydride (EDTAn), were treated with aqueous solutions of ibuprofen sodium salt (IbuNa) affording hydrogels that, after lyophilisation, gave two solid CDNS-drug formulations. (1)H fast MAS NMR and (13)C CP-MAS NMR spectra showed that IbuNa was converted in situ into its acidic and dimeric form (IbuH) after freeze-drying. (13)C CP-MAS NMR spectra also indicated that the structure of the nanosponge did not undergo changes upon drug loading compared to the unloaded system...
2017: Beilstein Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28228653/drug-prescription-appropriateness-in-the-elderly-an-italian-study
#19
Nicola Allegri, Federica Rossi, Federica Del Signore, Paolo Bertazzoni, Roberto Bellazzi, Giorgio Sandrini, Tomaso Vecchi, Davide Liccione, Alessia Pascale, Stefano Govoni
PURPOSE: Correct drug prescription in the elderly is a difficult task that requires careful survey of the current pharmacological therapies. In this article, we reviewed the drug prescriptions provided to 860 persons aged 65 years or over, residing in a small city of Lombardy, Italy. METHODS: Subjects were recruited from a local nursing home, the Pavia and Vigevano Neuropsychological Center for Alzheimer's Disease, general practitioners' offices, and the local University of the Third Age...
2017: Clinical Interventions in Aging
https://www.readbyqxmd.com/read/28228427/myocardial-infarction-risk-after-discontinuation-of-thienopyridine-therapy-in-the-randomized-dapt-study
#20
Ada C Stefanescu Schmidt, Dean J Kereiakes, Donald E Cutlip, Robert W Yeh, Ralph B D'Agostino, Joseph M Massaro, Wen-Hua Hsieh, Laura Mauri
Background -Thienopyridine plus aspirin beyond one year after coronary stenting (PCI) reduces myocardial infarction (MI) risk and increases bleeding risk compared with aspirin alone. The hazard associated with late thienopyridine discontinuation and risk factors for MI after discontinuation are poorly defined. Methods -In the Dual Antiplatelet Therapy (DAPT) Study, after PCI and 12 months of thienopyridine (clopidogrel or prasugrel) plus aspirin, eligible patients remained on aspirin and were randomized to continued thienopyridine vs...
February 22, 2017: Circulation
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