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https://www.readbyqxmd.com/read/28863863/unitary-properties-of-ampa-receptors-with-reduced-desensitization
#1
Wei Zhang, Clarissa Eibl, Autumn M Weeks, Irene Riva, Yan-Jun Li, Andrew J R Plested, James R Howe
Wild-type AMPA receptors display a characteristic rapidly desensitizing phenotype. Many studies point to the dimer interface between pairs of extracellular ligand binding domains as the key region controlling the rate at which the receptors desensitize. However, mutations at the extracellular end of the pore-forming regions (near the putative ion channel gate) have also been shown to alter desensitization. Here we report the behavior of single GluA4 receptors carrying one of two mutations that greatly reduce desensitization at the level of ensemble currents: the dimer interface mutation L484Y and the Lurcher mutation (A623T, GluA4-Lc) in the extracellular end of M3 (the second true transmembrane helix)...
August 30, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28836273/clotrimazole-microemulsion-and-microemulsion-based-gel-evaluation-of-buccal-drug-delivery-and-irritancy-using-chick-chorioallantoic-membrane-as-the-model
#2
Jarika Kaewbanjong, Paul Wan Sia Heng, Prapaporn Boonme
OBJECTIVES: To investigate the efficacy of clotrimazole microemulsion (CTZ-ME) and its gel form, clotrimazole microemulsion-based gel (CTZ-MBG), for the treatment of oral candidiasis. METHODS: CTZ-ME and CTZ-MBG were characterized for droplet size and texture, respectively. The ex-vivo permeation study and irritancy assessment of CTZ-ME and CTZ-MBG were performed using chick chorioallantoic membrane (CAM) as the model. Antifungal activity against Candida albicans ATCC 10 231 of CTZ-ME and CTZ-MBG was determined by agar diffusion method compared to the blank counterparts...
August 24, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28827351/mechanisms-of-synaptic-depression-at-the-hair-cell-ribbon-synapse-that-support-auditory-nerve-function
#3
Juan D Goutman
Inner hair cells (IHCs) in the cochlea are the mammalian phono-receptors, transducing sound energy into graded changes in membrane potentials, the so called "receptor potentials." Ribbon synapses between IHCs and auditory nerve neurons are responsible for converting receptor potentials into spike rates. The characteristics of auditory nerve responses to sound have been described extensively. For instance, persistent acoustic stimulation produces sensory adaptation, which is revealed as a reduction in neuronal spike rate with time constants in the range of milliseconds to seconds...
September 5, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28799218/synergy-and-mechanism-of-action-of-%C3%AE-mangostin-and-ceftazidime-against-ceftazidime-resistant-acinetobacter-baumannii
#4
T Pimchan, D Maensiri, G Eumkeb
To address the resistance of Acinetobacter baumannii to β-lactam antibiotics, combination therapy between different antibiotic classes is increasingly used. The antibacterial activity of α-mangostin (AMT) alone or in combination with ceftazidime (CTZ) was investigated against ceftazidime-resistant A. baumannii DMST 45378 (CRAB). Initial screening showed that A. baumannii strains possessed AmpC β-lactamase (AmpC), extended-spectrum beta-lactamase (ESBL) and metallo-β-lactamases (MBL). Minimum inhibitory concentrations (MICs) of all test agents were >800 μg ml(-1) against CRAB...
October 2017: Letters in Applied Microbiology
https://www.readbyqxmd.com/read/28771790/motoneuron-activity-is-required-for-enhancements-in-functional-recovery-after-peripheral-nerve-injury-in-exercised-female-mice
#5
Poonam B Jaiswal, Jack K Tung, Robert E Gross, Arthur W English
Inhibitory luminopsins (iLMO2) integrate opto- and chemo-genetic approaches and allow for cell-type specific inhibition of neuronal activity. When exposed to a Renilla luciferase substrate, Coelenterazine (CTZ), iLMO2 generates bioluminescence-mediated activation of its amino-terminal halorhodopsin, resulting in neuronal inhibition. Moderate daily exercise in the form of interval treadmill-training (IT) applied following a peripheral nerve injury results in enhanced motor axon regeneration and muscle fiber reinnervation in female mice...
August 3, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28732904/preparation-and-characterization-of-mucosal-adhesive-and-two-step-drug-releasing-cetirizine-chitosan-nanoparticle
#6
Xiaoping Yu, Yuzhi Mu, Mengxue Xu, Guixue Xia, Juan Wang, Ya Liu, Xiguang Chen
To develop a functional nanosized mucosal drug delivery system, a series of amphiphilic cetirizine-chitosan polymer (CTZ-CSs) were constructed. CTZ-CSs could self-assemble into nanoparticles (NPs) which gradually evolved from irregular aggregates to spherical particles with an increasing substitution degree (DS) in CTZ group. The average particle size of CTZ-CSs-NPs with nano ZS90 Zetasizer varied from 153.92nm to 184.48nm and their zeta potential varied between +19.14mV and +22.93mV. Biocompatibility assay exhibited CTZ-CS-NPs had few adverse effects within a certain concentration range...
October 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28623690/candidate-cytochrome-p450-genes-for-ethoxyresorufin-o-deethylase-activity-in-oyster-crassostrea-gigas
#7
Marília Nardelli Siebert, Jacó Joaquim Mattos, Guilherme Toledo-Silva, Guilherme Razzera, Afonso Celso Dias Bainy
Vertebrate cytochrome P450 1 (CYP1) enzymes metabolize endogenous and xenobiotic compounds and usually demonstrate a substrate-inducible response. Ethoxyresorufin O-deethylase activity (EROD) is a common method to quantify CYP1 enzymes activity in these organisms. Despite the absence of this gene family in protostomes, CYP1-like genes were identified in several species, even though no evolutionary relationship has been established with the vertebrate CYP1 family. In the present study, EROD activity was evaluated in microsomal fraction of gills, digestive gland and mantle of Crassostrea gigas...
August 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28601791/effect-of-operational-and-water-quality-parameters-on-conventional-ozonation-and-the-advanced-oxidation-process-o3-h2o2-kinetics-of-micropollutant-abatement-transformation-product-and-bromate-formation-in-a-surface-water
#8
Marc Bourgin, Ewa Borowska, Jakob Helbing, Juliane Hollender, Hans-Peter Kaiser, Cornelia Kienle, Christa S McArdell, Eszter Simon, Urs von Gunten
The efficiency of ozone-based processes under various conditions was studied for the treatment of a surface water (Lake Zürich water, Switzerland) spiked with 19 micropollutants (pharmaceuticals, pesticides, industrial chemical, X-ray contrast medium, sweetener) each at 1 μg L(-1). Two pilot-scale ozonation reactors (4-5 m(3) h(-1)), a 4-chamber reactor and a tubular reactor, were investigated by either conventional ozonation and/or the advanced oxidation process (AOP) O3/H2O2. The effects of selected operational parameters, such as ozone dose (0...
October 1, 2017: Water Research
https://www.readbyqxmd.com/read/28589389/-safety-and-efficacy-of-off-label-use-of-biologic-therapies-in-patients-with-inflammatory-rheumatic-diseases-refractory-to-standard-of-care-therapy-data-from-a%C3%A2-nationwide-german-registry-graid2
#9
F Proft, H Schulze-Koops, M Grunke, E Schrezenmeier, F Halleck, J Henes, L Unger, E Schmidt, C Fiehn, A Jacobi, C Iking-Konert, C Kneitz, R E Schmidt, B Bannert, R E Voll, R Fischer-Betz, I Kötter, H P Tony, J Holle, M Aringer, A Erler, F Behrens, G R Burmester, T Dörner
BACKGROUND: The German Registry of Autoimmune Diseases 2 (GRAID2) is a retrospective, non-interventional, multicenter registry study collecting data from patients with inflammatory, mainly rheumatic diseases refractory to standard of care therapy and treated with an off-label biologic therapy. The retrospective documentation comprised case history, diagnosis, course of disease (including safety and global efficacy). The objective was to evaluate the global clinical outcome and safety of off-label biologic therapy in clinical practice...
June 6, 2017: Zeitschrift Für Rheumatologie
https://www.readbyqxmd.com/read/28578237/ecotoxicity-of-the-antihistaminic-drug-cetirizine-to-ruditapes-philippinarum-clams
#10
Ângela Almeida, Vânia Calisto, Valdemar I Esteves, Rudolf J Schneider, Amadeu M V M Soares, Etelvina Figueira, Rosa Freitas
Cetirizine (CTZ) is an antihistaminic drug present in the aquatic environment, with limited information on its toxicity to organisms inhabiting this system. This study intended to evaluate the effects of CTZ on oxidative stress and energy metabolism biomarkers in the edible clam Ruditapes philippinarum after a 28days exposure to environmentally relevant CTZ concentrations (0.0, 0.3, 3.0, 6.0 and 12.0μg/L). The results obtained showed that CTZ was accumulated by clams reaching maximum concentrations (up to ~22ng/g FW) at the highest CTZ exposure concentrations (6...
December 1, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28424463/luciferase-specific-coelenterazine-analogues-for-optical-contamination-free-bioassays
#11
Ryo Nishihara, Masahiro Abe, Shigeru Nishiyama, Daniel Citterio, Koji Suzuki, Sung Bae Kim
Spectral overlaps among the multiple optical readouts commonly cause optical contamination in fluorescence and bioluminescence. To tackle this issue, we created five-different lineages of coelenterazine (CTZ) analogues designed to selectively illuminate a specific luciferase with unique luciferase selectivity. In the attempt, we found that CTZ analogues with ethynyl or styryl groups display dramatically biased bioluminescence to specific luciferases and pHs by modifying the functional groups at the C-2 and C-6 positions of the imidazopyradinone backbone of CTZ...
April 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28259787/development-of-a-common-carp-cyprinus-carpio-pregnane-x-receptor-cpxr-transactivation-reporter-assay-and-its-activation-by-azole-fungicides-and-pharmaceutical-chemicals
#12
Anke Lange, Jenna Corcoran, Shinichi Miyagawa, Taisen Iguchi, Matthew J Winter, Charles R Tyler
In mammals, the pregnane X receptor (PXR) is a transcription factor with a key role in regulating expression of several genes involved in drug biotransformation. PXR is present in fish and some genes known to be under its control can be up-regulated by mammalian PXR ligands. Despite this, direct involvement of PXR in drug biotransformation in fish has yet to be established. Here, the full length PXR sequence was cloned from carp (Cyprinus carpio) and used in a luciferase reporter assay to elucidate its role in xenobiotic metabolism in fish...
June 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28228057/intravenous-chlorothiazide-versus-enteral-metolazone-to-augment-loop-diuretic-therapy-in-the-intensive-care-unit
#13
Christopher J Michaud, Kendall C Mintus
BACKGROUND: In cases of loop diuretic resistance in the intensive care unit (ICU), recommendations for a specific second-line thiazide agent are lacking. OBJECTIVE: To compare the effects of intravenous chlorothiazide (CTZ) and enteral metolazone (MET) on urine output (UOP) when added to furosemide monotherapy therapy in critically ill adults. METHODS: This was a retrospective cohort study conducted in the medical, surgical, and cardiothoracic ICUs of a quaternary medical center...
April 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/27702426/burkholderia-pseudomallei-resistance-to-antibiotics-in-biofilm-induced-conditions-is-related-to-efflux-pumps
#14
Nopphasul Sirijant, Rasana W Sermswan, Surasakdi Wongratanacheewin
Burkholderia pseudomallei, the causative agent of melioidosis, has been found to increase its resistance to antibiotics when growing as a biofilm. The resistance is related to several mechanisms. One of the possible mechanisms is the efflux pump. Using bioinformatics analysis, it was found that BPSL1661, BPSL1664 and BPSL1665 were orthologous genes of the efflux transporter encoding genes for biofilm-related antibiotic resistance, PA1874-PA1877 genes in Pseudomonas aeruginosa strain PAO1. Expression of selected encoding genes for the efflux transporter system during biofilm formation were investigated...
November 2016: Journal of Medical Microbiology
https://www.readbyqxmd.com/read/27574791/effect-of-chitosan-coating-on-microemulsion-for-effective-dermal-clotrimazole-delivery
#15
Babita Kumari, Karthikeyan Kesavan
Clotrimazole (CTZ) is a broad spectrum antimycotic agent known to be very effective locally for the treatment of fungal skin infections. The aim of this study was to study the effect of chitosan-coated microemulsion (CME) for topical delivery of CTZ and also evaluate its in vitro antifungal efficacy, ex vivo permeation and retention ability on the skin surface. The pseudo-ternary phase diagrams were developed using clove oil as oil phase, Tween 80 and propylene glycol as surfactant and co-surfactant, respectively, and distilled water as aqueous phase...
June 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27472562/endodontic-treatment-of-primary-molars-with-antibiotic-paste-a-report-of-38-cases
#16
Lúcia de Fátima Almeida de Deus Moura, Marina de Deus Moura de Lima, Cacilda Castelo Branco Lima, Jessa Iashmin Alcobaça Gomes Machado, Marcoeli Silva de Moura, Paulo Vasconcelos de Carvalho
OBJECTIVE: This study presents 38 cases of primary molars with necrotic pulps treated with antibiotics-based paste. CASE REPORT: The technique consisted of necrotic tissue removal of the pulp chamber, using spoons excavators and low speed drills. Pulp cavity was washed with saline solution and dried with sterile cotton balls. Then an antibiotic paste composed of chloramphenicol, tetracycline, zinc oxide and eugenol - CTZ paste - was inserted at the entrance of root canals...
2016: Journal of Clinical Pediatric Dentistry
https://www.readbyqxmd.com/read/27424892/synthetic-bioluminescent-coelenterazine-derivatives
#17
Ryo Nishihara, Daniel Citterio, Koji Suzuki
The development of coelenterazine (CTZ) derivatives resulting in superior optical characteristics is an efficient method to extend the range of its possible applications. Here, we describe the synthesis of three C-6 substituted CTZ derivatives retaining the recognition by Renilla luciferase (RLuc) and its derivatives. The novel derivatives are useful as bright blue-shifted CTZ derivatives, which can be used as an alternative to hitherto reported compound DeepBlueC™.
2016: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27383651/ru-ii-clotrimazole-diphenylphosphine-bipyridine-complexes-interaction-with-dna-bsa-and-biological-potential-against-tumor-cell-lines-and-mycobacterium-tuberculosis
#18
Legna Colina-Vegas, Jocely Lucena Dutra, Wilmer Villarreal, João Honorato de A Neto, Marcia Regina Cominetti, Fernando Pavan, Maribel Navarro, Alzir A Batista
Three ruthenium complexes [RuCl(CTZ)(bipy)(P-P)]PF6 [P-P=1,2-bis(diphenylphosphino)ethane (dppe-1), 1,4-bis(diphenylphosphino)butane (dppb-2) and 1,1'-bis(diphenylphosphino)ferrocene (dppf-3), bipy=2,2'-bipiridine and clotrimazole (CTZ) 1-[(2-chlorophenyl)diphenylmethyl]-1H-imidazole] were synthesized. These complexes were characterized by a combination of elemental analysis, molar conductivity, infrared and UV-vis spectroscopy, (1)H, (13)C{(1)H} and (31)P{(1)H} nuclear magnetic resonance techniques, cyclic voltammetry and mass spectroscopy...
September 2016: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/27376373/efficacy-and-treatment-costs-of-monotherapy-with-bdmards-in-the-treatment-of-rheumatoid-arthritis-in-patients-intolerant-to-or-inappropriate-to-continue-treatment-with-methotrexate
#19
RANDOMIZED CONTROLLED TRIAL
Alberto Batticciotto, Roberto Ravasio, Marta Riva, Piercarlo Sarzi-Puttini
INTRODUCTION: Only limited information is available on cost efficacy of the various biological agents used to treat patients with rheumatoid arthritis with intolerance or for whom it would be inappropriate to continue treatment with conventional agents. We estimated the efficacy and treatment costs of monotherapy with biological agents in the treatment of this group of patients. METHODS: Data from two previous meta-analyses in the treatment of patients who are intolerant to methotrexate (MTX), or for whom it would be inappropriate to continue treatment with MTX was used...
August 2016: Advances in Therapy
https://www.readbyqxmd.com/read/27317297/extended-therapeutic-window-of-a-novel-peptide-inhibitor-of-trpm2-channels-following-focal-cerebral-ischemia
#20
Takeru Shimizu, Robert M Dietz, Ivelisse Cruz-Torres, Frank Strnad, Ana K Garske, Myriam Moreno, Venugopal R Venna, Nidia Quillinan, Paco S Herson
INTRODUCTION: TRPM2 channels have been suggested to play a role in ischemic neuronal injury, specifically in males. A major hindrance to TRPM2 research has been the lack of specific TRPM2 inhibitors. The current study characterized the specificity and neuroprotective efficacy of a novel TRPM2 inhibitor. METHODS: Fluorescent calcium imaging (Fluo5F) was used to determine inhibitor efficacy of the TRPM2 peptide inhibitor (tat-M2NX) in HEK293 cells stably expressing hTRPM2...
September 2016: Experimental Neurology
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