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https://www.readbyqxmd.com/read/28088085/new-pyridazinone-4-carboxamides-as-new-cannabinoid-receptor-type-2-inverse-agonists-synthesis-pharmacological-data-and-molecular-docking
#1
Giulio Ragusa, María Gómez-Cañas, Paula Morales, Carmen Rodríguez-Cueto, María R Pazos, Battistina Asproni, Elena Cichero, Paola Fossa, Gerard A Pinna, Nadine Jagerovic, Javier Fernández-Ruiz, Gabriele Murineddu
In the last few years, cannabinoid type-2 receptor (CB2R) selective ligands have shown a great potential as novel therapeutic drugs in several diseases. With the aim of discovering new selective cannabinoid ligands, a series of pyridazinone-4-carboxamides was designed and synthesized, and the new derivatives tested for their affinity toward the hCB1R and hCB2R. The 6-(4-chloro-3-methylphenyl)-2-(4-fluorobenzyl)-N-(cis-4-methylcyclohexyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide (9) displayed high CB2-affinity (KiCB2 = 2...
January 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28087976/the-role-of-diode-array-ultraviolet-detection-for-the-identification-of-synthetic-cathinones
#2
Walter F Rowe, Ioan Marginean, Stephanie Carnes, Ira S Lurie
The utility of diode array UV detection for aiding in the identification of synthetic cathinones, including different sub classes and positional isomers is presented. For 35 synthetic cathinones' unique UV spectra are obtained for seven sub classes including mostly beta ketones, where position and type of substitution on benzene rings give rise to differences in UV maxima and relative intensity of the spectral bands. This aspect is key to distinguishing positional isomers which contain differences in R substitution (mono and di) around the benzene ring, which provides complementary information to electron ionization mass spectrometry, where the latter technique cannot distinguish between these types of positional isomers...
January 14, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28087819/electrophysiologic-effects-of-the-ik1-inhibitor-pa-6-are-modulated-by-extracellular-potassium-in-isolated-guinea-pig-hearts
#3
Gregory S Hoeker, Mark A Skarsfeldt, Thomas Jespersen, Steven Poelzing
The pentamidine analog PA-6 was developed as a specific inward rectifier potassium current (IK1) antagonist, because established inhibitors either lack specificity or have side effects that prohibit their use in vivo. We previously demonstrated that BaCl2, an established IK1 inhibitor, could prolong action potential duration (APD) and increase cardiac conduction velocity (CV). However, few studies have addressed whether targeted IK1 inhibition similarly affects ventricular electrophysiology. The aim of this study was to determine the effects of PA-6 on cardiac repolarization and conduction in Langendorff-perfused guinea pig hearts...
January 2017: Physiological Reports
https://www.readbyqxmd.com/read/28087784/interactions-between-zinc-and-allosteric-modulators-of-the-glycine-receptor
#4
Garrett L Cornelison, Anna W Daszkowski, Natasha C Pflanz, S John Mihic
The glycine receptor is a pentameric ligand-gated ion channel involved in fast inhibitory neurotransmission in the central nervous system. Zinc is an allosteric modulator of glycine receptor function, enhancing the effects of glycine at nM to low μM concentrations, and inhibiting its effects at higher concentrations. Low nM concentrations of contaminating zinc in electrophysiological buffers are capable of synergistically enhancing receptor modulation by other compounds such as ethanol. This suggests that, unless accounted for, previous studies of glycine receptor modulation were measuring the effects of modulator plus co-modulation by zinc on receptor function...
January 13, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28087520/atheroprotective-vaccination-with-mhc-ii-restricted-apob-peptides-induces-peritoneal-il-10-producing-cd4-t-cells
#5
Takayuki Kimura, Kevin Tse, Sara McArdle, Teresa Gerhardt, Jacqueline Miller, Zbigniew Mikulski, John Sidney, Alessandro Sette, Dennis Wolf, Klaus Ley
Although immunization with MHC class II-restricted ApoB peptides has been shown to be atheroprotective, the mechanism is unclear. Here, we investigated CD4(+) T cell populations in immunized atherosclerotic mice. Peptides (16-mers) from mouse ApoB, the core protein of low-density lipoprotein (LDL), were screened for binding to I-A(b) by computer prediction and confirmed by radiolabeled peptide competition. Three new peptides, P101 (FGKQGFFPDSVNKALY, 5.5 nM IC50), P102 (TLYALSHAVNSYFDVD, 6.8 nM), and P103 (LYYKEDKTSLSASAAS, 95 nM) were tested in an atherosclerosis model (Apoe(-/-) mice on western diet)...
January 13, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/28087484/inhibition-of-bacterial-adhesion-and-biofilm-formation-by-dual-functional-textured-and-nitric-oxide-releasing-surfaces
#6
Li-Chong Xu, Yaqi Wo, Mark E Meyerhoff, Christopher A Siedlecki
: In separate prior studies, physical topographic surface modification or nitric oxide (NO) release has been demonstrated to each be an effective approach to inhibit and control bacterial adhesion and biofilm formation on polymeric surfaces. Such approaches can prevent biomaterial-associated infection without causing the antibiotic resistance of the strain. In this work, both techniques were successfully integrated and applied to a polyurethane (PU) biomaterial surface that bears ordered pillar topographies (400/400 nm and 500/500 nm patterns) at the top surface and a S-nitroso-N-acetylpenicillamine (SNAP, NO donor) doped sub-layer in the middle, via a soft lithography two-stage replication process...
January 10, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28087379/pegylated-liposomes-for-topical-vaginal-therapy-improve-delivery-of-interferon-alpha
#7
May Wenche Jøraholmen, Purusotam Basnet, Ganesh Acharya, Nataša Škalko-Basnet
Recent studies regarding mucosal drug delivery indicate that nanosystems with surface-available polyethylene glycol (PEG) are able to penetrate mucus barrier, assure closer contact with the epithelium, and improve drug delivery to vagina. In the present work, we developed the mucus-penetrating PEGylated liposomes containing interferon alpha-2b (IFN α-2b), destined to provide localized therapy for human papilloma virus (HPV) vaginal infections. The PEGylated liposomes were of a mean size of 181 ± 8 nm, bearing a negative zeta potential of - 13 mV and an entrapment efficiency of 81 ± 10 %...
January 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087337/tunicamycin-impairs-olfactory-learning-and-synaptic-plasticity-in-the-olfactory-bulb
#8
Jia Tong, Fumino Okutani, Yoshihiro Murata, Mustuo Taniguchi, Toshiharu Namba, Yu-Jie Wang, Hideto Kaba
Tunicamycin (TM) induces endoplasmic reticulum (ER) stress and inhibits N-glycosylation in cells. ER stress is associated with neuronal death in neurodegenerative disorders, such as Parkinson's disease and Alzheimer's disease, and most patients complain of the impairment of olfactory recognition. Here we examined the effects of TM on aversive olfactory learning and the underlying synaptic plasticity in the main olfactory bulb (MOB). Behavioral experiments demonstrated that the intrabulbar infusion of TM disabled aversive olfactory learning without affecting short-term memory...
January 10, 2017: Neuroscience
https://www.readbyqxmd.com/read/28086963/near-infrared-spectroscopy-for-body-fat-sensing-in-neonates-quantitative-analysis-by-gamos-simulations
#9
Fatin Hamimi Mustafa, Peter W Jones, Alistair L McEwan
BACKGROUND: Under-nutrition in neonates is closely linked to low body fat percentage. Undernourished neonates are exposed to immediate mortality as well as unwanted health impacts in their later life including obesity and hypertension. One potential low cost approach for obtaining direct measurements of body fat is near-infrared (NIR) interactance. The aims of this study were to model the effect of varying volume fractions of melanin and water in skin over NIR spectra, and to define sensitivity of NIR reflection on changes of thickness of subcutaneous fat...
January 11, 2017: Biomedical Engineering Online
https://www.readbyqxmd.com/read/28086858/the-influence-of-adding-modified-zirconium-oxide-titanium-dioxide-nano-particles-on-mechanical-properties-of-orthodontic-adhesive-an-in-vitro-study
#10
Nayef H Felemban, Mohamed I Ebrahim
BACKGROUND: The purpose of this in-vitro study was to examine the effect of incorporating different concentrations of Zirconium oxide-Titanium dioxide (ZrO2-TiO2) nanoparticles, which can have antibacterial properties, on the mechanical properties of an orthodontic adhesive. METHODS: ZrO2-TiO2 (Zirconium oxide, HWNANO, Hongwu International Group Ltd, China) -Titanium dioxide, Nanoshell, USA) nanopowder were incorporated into orthodontic adhesive (Transbond XT, 3 M Unitek, Monrovia, USA) with different concentrations (0...
January 13, 2017: BMC Oral Health
https://www.readbyqxmd.com/read/28081367/ordered-mesoporous-titanium-nitride-as-a-promising-carbon-free-cathode-for-aprotic-lithium-oxygen-batteries
#11
Byung Gon Kim, Changshin Jo, Jaeho Shin, Yeongdong Mun, Jinwoo Lee, Jang Wook Choi
Despite the extraordinary gravimetric energy densities, Li-O2 batteries are still facing a technological challenge; limited round trip efficiency leading to insufficient cycle life. Recently, carbonaceous electrode materials were found to be one of the primary origins of the limited cycle life, as they produce irreversible side products during discharge. A few investigations based on non-carbonaceous materials have demonstrated largely suppressed accumulation of irreversible side products but such studies have focused mainly on the materials themselves rather than delicate morphology control...
January 12, 2017: ACS Nano
https://www.readbyqxmd.com/read/28081299/ultrasound-detection-of-regional-oxidative-stress-in-deep-tissues-using-novel-enzyme-loaded-nanoparticles
#12
Emilia S Olson, Inanc Ortac, Christopher Malone, Sadik Esener, Robert Mattrey
Oxidative stress is a powerful tool that is critical to immune mediated responses in healthy individuals, yet additionally plays a crucial role in development of cancer, inflammatory pathologies, and tissue ischemia. Despite this, there remain relatively few molecular tools to study oxidative stress, particularly in living mammals. To develop an intravenously injectable probe capable of labeling sites of oxidative stress in vivo, 200 nm catalase synthetic hollow enzyme loaded nanospheres (catSHELS) are designed and fabricated using a versatile enzyme nanoencapsulation method...
January 12, 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/28081257/influence-of-la3-substitution-on-structure-morphology-and-magnetic-properties-of-nanocrystalline-ni-zn-ferrite
#13
Y K Dasan, B H Guan, M H Zahari, L K Chuan
Lanthanum substituted Ni-Zn ferrite nanoparticles (Ni0.5Zn0.5LaxFe1-xO4; 0.00 ≤x≤ 1.00) synthesized by sol-gel method were presented. X-ray diffraction patterns reveal the typical single phase spinel cubic ferrite structure, with the traces of secondary phase for lanthanum substituted nanocrystals. In addition, the structural analysis also demonstrates that the average crystallite size varied in the range of 21-25 nm. FTIR spectra present the two prominent absorption bands in the range of 400 to 600 cm-1 which are the fingerprint region of all ferrites...
2017: PloS One
https://www.readbyqxmd.com/read/28081255/changes-in-dna-methylation-in-mouse-lungs-after-a-single-intra-tracheal-administration-of-nanomaterials
#14
Ali M Tabish, Katrien Poels, Hyang-Min Byun, Katrien Luyts, Andrea A Baccarelli, Johan Martens, Stef Kerkhofs, Sven Seys, Peter Hoet, Lode Godderis
AIMS: This study aimed to investigate the effects of nanomaterial (NM) exposure on DNA methylation. METHODS AND RESULTS: Intra-tracheal administration of NM: gold nanoparticles (AuNPs) of 5-, 60- and 250-nm diameter; single-walled carbon nanotubes (SWCNTs) and multi-walled carbon nanotubes (MWCNTs) at high dose of 2.5 mg/kg and low dose of 0.25 mg/kg for 48 h to BALB/c mice. Study showed deregulations in immune pathways in NM-induced toxicity in vivo. NM administration had the following DNA methylation effects: AuNP 60 nm induced CpG hypermethylation in Atm, Cdk and Gsr genes and hypomethylation in Gpx; Gsr and Trp53 showed changes in methylation between low- and high-dose AuNP, 60 and 250 nm respectively, and AuNP had size effects on methylation for Trp53...
2017: PloS One
https://www.readbyqxmd.com/read/28081106/broad-bandwidth-reversible-and-high-contrast-ratio-optical-diode
#15
Chao Li, Min Wang, Jun-Fang Wu
Fano resonance is widely used to realize high-contrast nonreciprocal transmission. However, resonance-enhanced all-optical diodes (AOD) are bandwidth-limited, and their transmission rates are normally low, which restricts realistic application. In this Letter, we analytically and numerically demonstrate that this limitation can be overcome once multistability of cascaded nonlinear cavities is appropriately excited. By precisely molding the transiting of the signal light between multistable states, a high-contrast-ratio, high-unidirectional-transmission-rate, and reversal-controllable AOD is achieved with a bandwidth over 2...
January 15, 2017: Optics Letters
https://www.readbyqxmd.com/read/28081098/generation-of-terahertz-optical-beating-from-a-simultaneously-self-mode-locked-nd-yag-laser-at-1064-and-1123%C3%A2-%C3%A2-nm
#16
C L Sung, C Y Lee, C C Chang, H C Liang, Y F Chen
The reflectivity of the output coupler is designed to achieve the synchronously self-mode-locked operation at 1064 and 1123 nm in a diode-end-pumped Nd:YAG laser. Numerical analyses are performed to confirm that the designed output coupler can lead the emission lines to be predominant at 1064 and 1123 nm. Moreover, the crossover of the threshold pump powers for the 1064 and 1123 nm emission lines can be exploited to obtain the single central wavelength of 1064 nm or the single central wavelength of 1123 nm or, simultaneously, dual-central-wavelength self-mode-locked operation by finely adjusting the cavity alignment...
January 15, 2017: Optics Letters
https://www.readbyqxmd.com/read/28081090/enhancement-cavities-for-few-cycle-pulses
#17
N Lilienfein, C Hofer, S Holzberger, C Matzer, P Zimmermann, M Trubetskov, V Pervak, I Pupeza
We address the challenge of increasing the bandwidth of high-finesse femtosecond enhancement cavities and demonstrate a broad spectrum spanning 1800  cm<sup>-1</sup> (195 nm) at -10  dB around a central wavelength of 1050 nm in an EC with an average finesse exceeding 300. This will benefit a host of spectroscopic applications, including transient absorption spectroscopy, direct frequency comb spectroscopy, and Raman spectroscopy. The pulse circulating in the EC is composed of only 5.4 optical cycles, at a kilowatt-level average power...
January 15, 2017: Optics Letters
https://www.readbyqxmd.com/read/28081082/seedless-velocimetry-at-100%C3%A2-%C3%A2-khz-with-picosecond-laser-electronic-excitation-tagging
#18
Naibo Jiang, Jason G Mance, Mikhail N Slipchenko, Josef J Felver, Hans U Stauffer, Tongxun Yi, Paul M Danehy, Sukesh Roy
Picosecond-laser electronic-excitation tagging (PLEET), a seedless picosecond-laser-based velocimetry technique, is demonstrated in non-reactive flows at a repetition rate of 100 kHz with a 1064 nm, 100 ps burst-mode laser. The fluorescence lifetime of the PLEET signal was measured in nitrogen, and the laser heating effects were analyzed. PLEET experiments with a free jet of nitrogen show the ability to measure multi-point flow velocity fluctuations at a 100 kHz detection rate or higher. Both spectral and dynamic mode decomposition analyses of velocity on a Ma=0...
January 15, 2017: Optics Letters
https://www.readbyqxmd.com/read/28081081/compact-broadband-polarization-beam-splitter-using-a-symmetric-directional-coupler-with-sinusoidal-bends
#19
Fan Zhang, Han Yun, Yun Wang, Zeqin Lu, Lukas Chrostowski, Nicolas A F Jaeger
We design and demonstrate a compact broadband polarization beam splitter (PBS) using a symmetric directional coupler with sinusoidal bends on a silicon-on-insulator platform. The sinusoidal bends in our PBS suppress the power exchange between two parallel symmetric strip waveguides for the transverse-electric (TE) mode, while allowing for the maximum power transfer to the adjacent waveguide for the transverse-magnetic (TM) mode. Our PBS has a nominal coupler length of 8.55 μm, and it has an average extinction ratio (ER) of 12...
January 15, 2017: Optics Letters
https://www.readbyqxmd.com/read/28081076/spatially-resolved-individual-particle-spectroscopy-using-photothermal-modulation-of-mie-scattering
#20
R M Sullenberger, S M Redmond, D Crompton, A M Stolyarov, W D Herzog
We report a photothermal modulation of Mie scattering (PMMS) method that enables concurrent spatial and spectral discrimination of individual micron-sized particles. This approach provides a direct measurement of the "fingerprint" infrared absorption spectrum with the spatial resolution of visible light. Trace quantities (tens of picograms) of material were deposited onto an infrared-transparent substrate and simultaneously illuminated by a wavelength-tunable intensity-modulated quantum cascade pump laser and a continuous-wave 532 nm probe laser...
January 15, 2017: Optics Letters
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