bluuebunny/crossref_metadata_2025_split huggingface dataset:
In vitro pharmacological characterization of a novel unbiased NOP receptor‐selective nonpeptide agonist AT‐403
Authors: Ferrari Federica , Malfacini Davide , Journigan Blair V. , Bird Mark F. , Trapella Claudio , Guerrini Remo , Lambert David G. , Calo' Girolamo , Zaveri Nurulain T. 
Published: July 2017

AbstractNociceptin/orphanin FQ (N/OFQ) regulates several biological functions via selective activation of the N/OFQ receptor (NOP), a member of the opioid receptor family. We recently identified a new high affinity and highly selective NOP agonist AT‐403. In this study, we characterized the functional profile of AT‐403 and compared it to other known nonpeptide NOP agonists Ro 65‐6570, Ro 2q, SCH‐221510, MCOPPB, AT‐202 and SCH‐486757, using the following assays: GTPγ[35S] stimulated binding, calcium mobilization assay in cells‐expressing human NOP or classical opioid receptors and chimeric G proteins, bioluminescence resonance energy transfer (BRET) based assay for studying NOP receptor interaction with G protein and arrestin, and the electrically stimulated mouse vas deferens bioassay. All compounds behaved as NOP full agonists consistently showing the following rank order of potency MCOPPB > AT‐403 > Ro 65‐6570 = Ro 2q > SCH‐221510 > AT‐202 > SCH‐486757. AT‐403 and MCOPPB displayed the highest NOP selectivity both at human and murine receptors. Interestingly, while all the other nonpeptide NOP agonists displayed bias toward G protein‐mediated signaling in the BRET assay, AT‐403, similar to the natural ligand N/OFQ, behaved as an unbiased agonist, activating G‐protein‐mediated function as well as arrestin recruitment. AT‐403 may be a useful nonpeptide tool compound to study the pharmacology of NOP activation in disease states.
Polymerization of 1‐(2‐Propynyl)‐3‐methylimidazolium Bromide using Cyclometalated Pd(II) Catalysts and Study of the Interaction of Ensuing Oligomer with BSA
Authors: Mukhopadhyay Sujay , Mitra Kheyanath , Paitandi Rajendra Prasad , Singh Roop Shikha , Singh Shikha , Ray Biswajit , Pandey Daya Shankar 
Published: July 2017

AbstractTwo novel cyclometalated binuclear chloro‐bridged palladium based catalysts, {(PdClL1)2} (1) and {(PdClL2)2} (2) have been synthesized by reacting PdCl2 with 4‐nitro‐(benzylidene‐(4‐tert‐butyl‐phenyl)‐amine (L1) and 4‐methylester‐(benzylidene‐(4‐tert‐butyl‐phenyl)‐amine (L2), respectively. These have been characterized by elemental analyses, spectroscopic studies (IR, 1H, 13C NMR, ESI‐MS), and their structures have been authenticated by X‐ray single crystal analyses. Polymerization of ionic liquid monomer using these catalysts has been investigated. 1 exhibited best catalytic activity and each catalyst afforded both conducting and fluorescent oligomers and high molecular weight polymers. Resulting oligomers and polymers have been characterized by spectroscopic and conductivity, GPC, SEM‐EDAX, PXRD studies. Oligomers are fluorescent and their emission intensity enhances upon interaction with anions. Binding behaviour of oligomers has been examined with BSA. Quenching of the intrinsic fluorescence of BSA in presence of oligomers have been studied by steady state, synchronous, and 3D fluorescence spectroscopy and changes in secondary structure quantified by CD spectroscopy.
Effects of Multiple Factors on Methane Hydrate Reformation in a Porous Medium
Authors: Wang Pengfei , Yang Mingjun , Jiang Lanlan , Zhao Yuechao , Song Yongchen 
Published: July 2017

AbstractThe effects of the remaining hydrate saturation (remaining Sh), reformation pressure and methane flow velocity on methane hydrate (MH) reformation in a porous medium were investigated. The results indicate that the presence of residual hydrate affects the hydrate reformation distribution. The remaining Sh has a more obvious effect on the hydrate reformation saturation than the pressure and methane flow velocity during the rapid reformation stage. However, in the stable reformation stage, the pressure has the largest effect on the hydrate reformation saturation. In addition, the increases in reformation Sh are related to the remaining Sh, and the remaining Sh has a negative effect on the Sh increment. A comparison of the hydrate reformation rates at various times suggests that both reformation pressure and remaining Sh affect the hydrate reformation rate. The remaining Sh has a more remarkable effect than the reformation pressure. In addition, the maximum hydrate reformation rate is related to the remaining Sh, and the maximum hydrate reformation rate will decrease when the level of remaining Sh increases.
Self‐Assembly of Solution‐Processable Polyindole via Langmuir‐Blodgett Technique: An Insight to Layer‐Dependent Charge Transport and Electronic Parameters
Authors: Mishra Richa , Pandey Rajiv K. , Upadhyay Chandan , Prakash Rajiv 
Published: July 2017

AbstractOrdering of polymer chains at molecular level using a suitable post‐synthesis fabrication technique is highly motivating towards enhancement in performance of organic electronic devices. Here, we report the formation of stable, large area self‐assembled Langmuir‐Blodgett (LB) films of unsubstituted polyindole (PIn) without aid of any surfactant. Pressure vs Area (π‐A) isotherm for PIn is studied prior to device fabrication. Investigation of film uniformity via atomic force microscopy and scanning electron microscopy justified 30 mN/m as optimum surface pressure for depositing large area PIn LB films. Self‐assembly in LB film is confirmed by absorption and Raman spectroscopy before device fabrication. A layer dependent charge transport of LB film of PIn is studied via current density (J)–voltage (V) characteristics and subsequently various device parameters are extracted using Schottky diode configuration of sandwiched structure Al/PIn LB film/ITO. A deviation in ideality factor, rectification ratio, current density and barrier height is observed for different number of layers. The electrical characteristics are also discussed taking into account the absorption spectra, Raman spectra, surface morphology, topography, barrier height. This study shows enormous potential for the fabrication of ordered PIn polymer on large area based electronic device application.
Synthesis and Characterisation of Fused Heterocyclic Molecular Rods: A Combined Experimental and Theoretical Study on Diethynyl Dithienothiophenyl Derivatives
Authors: Jones Leighton , Pask Christopher M. , Kazlauciunas Algy , Gulcur Murat , Lin Long 
Published: July 2017

AbstractA structural and electronic diversity of symmetric diethynyl dithienothiophenyl (DTT) molecular rods were synthesised and their properties fully characterised using optical and thermal analysis and complemented with density functional theory (DFT) calculations. It was found that some structures are stable up to 381 °C. Due to the nature of both the derivative and the substituent, physical properties such as electron donating ability and thermal stability can be fine‐tuned to generate rationally designed materials, all of which have excellent solubility in common organic solvents. The single‐crystal x‐ray structures revealed that both bulky silyl and linear alkyl derivatives generate regular lateral close packing between the adjacent molecules, suitable for charge‐transfer in organic thin‐film transistors (OTFTs), whereas the same ethynyl derivative without an alkyl chain gives a non‐planar interlinking structure and thus unsuitable for OTFTs. These air‐stable electron rich DTT‐based molecular rods have strong potential as organic semiconductors for organic electronic applications.
A Luminescent Perylenediimide as a Binding Ligand for Pyrimidine/Pyrimidine Mismatches Within a DNA Duplex
Authors: Takada Tadao , Umakoshi Yu , Nakamura Mitsunobu , Yamana Kazushige 
Published: July 2017

AbstractSynthetic small molecules with a binding affinity to mismatched base pairs have been widely studied because of their potential applications in chemotherapeutic drugs and diagnostic tools for the detection of single nucleotide variations. In this paper, a luminescent ligand, a perylenediimide (PO) derivative, which is capable of binding to mismatched base pairs within a DNA duplex and generating a strong fluorescence upon the binding event, was demonstrated. Fluorescence enhancement of PO upon the binding to pyrimidine/pyrimidine mismatches were prominent and reached ca. 100‐fold for a C/C mismatched base pair, which was visually observed. This result represents the best performance as a fluorescence turn‐on response among the existing mismatch binding ligands.
In Vivo Rescue of the Hematopoietic Niche By Pluripotent Stem Cell Complementation of Defective Osteoblast Compartments
Authors: Chubb Rhiannon , Oh James , Riley Alyssa K. , Kimura Takaharu , Wu Sean M. , Wu Joy Y. 
Published: July 2017

Abstract
Bone-forming osteoblasts play critical roles in supporting bone marrow hematopoiesis. Pluripotent stem cells (PSCs), including embryonic stem cells (ESCs) and induced PSCs (iPSC), are capable of differentiating into osteoblasts. To determine the capacity of stem cells needed to rescue aberrant skeletal development and bone marrow hematopoiesis in vivo, we used a skeletal complementation model. Mice deficient in Runx2, a master transcription factor for osteoblastogenesis, fail to form a mineralized skeleton and bone marrow. Wild-type (WT) green fluorescent protein (GFP)+ ESCs and yellow fluorescent protein (YFP)+ iPSCs were introduced into Runx2-null blastocyst-stage embryos. We assessed GFP/YFP+ cell contribution by whole-mount fluorescence and histological analysis and found that the proportion of PSCs in the resulting chimeric embryos is directly correlated with the degree of mineralization in the skull. Moreover, PSC contribution to long bones successfully restored bone marrow hematopoiesis. We validated this finding in a separate model with diphtheria toxin A-mediated ablation of hypertrophic chondrocytes and osteoblasts. Remarkably, chimeric embryos harboring as little as 37.5% WT PSCs revealed grossly normal skeletal morphology, suggesting a near-complete rescue of skeletogenesis. In summary, we demonstrate that fractional contribution of PSCs in vivo is sufficient to complement and reconstitute an osteoblast-deficient skeleton and hematopoietic marrow. Further investigation using genetically modified PSCs with conditional loss of gene function in osteoblasts will enable us to address the specific roles of signaling mediators to regulate bone formation and hematopoietic niches in vivo.
Assessment of diastolic function of normal fetal heart using dual‐gate Doppler
Authors: Takano M. , Nakata M. , Nagasaki S. , Ueyama R. , Morita M. 
Published: July 2017

ABSTRACTObjectivesThe ratio of mitral peak early diastolic filling to early diastolic mitral annular velocity (E/e′) reflects diastolic cardiac function in adults. Dual‐gate Doppler (DD) enables measurements of E/e′ in the same heart beat. This study was designed to assess the utility of the DD method for measurement of fetal E/e′ and determine reference ranges for normal fetuses.MethodsThis prospective study comprised normal singleton pregnancies undergoing fetal echocardiography between 16 and 36 weeks of gestation. According to the DD method, E‐wave velocity on pulsed‐wave Doppler and e′‐wave on tissue Doppler imaging were measured simultaneously on an apical or basal four‐chamber view, and fetal E/e′ was calculated. Spearman's correlation coefficient was used to assess the relationship between gestational age (GA) and E‐wave and e′‐wave velocities and E/e′.ResultsA total of 133 pregnancies were included in this study and all E/e′ measurements were successful. Significant correlation was observed between GA and both left ventricular (LV) E/e′ (r
s = –0.666, P < 0.001) and right ventricular (RV) E/e′ (r
s = –0.607, P < 0.001). The regression equations for bilateral E/e′ were: LV‐E/e′ = 17.341 − 0.631GA + 0.008 × GA2 (mean ± SD, R
2 = 0.440 ± 1.333); and RV‐E/e′ = 19.156 − 0.794GA + 0.012GA2 (R
2 = 0.419 ± 1.329).ConclusionsBilateral E/e′ of normal fetuses, measured using the DD method, decreased with GA, which is considered to be related to myocardial maturity. DD is a useful and convenient method for evaluating fetal E/e′ in order to assess diastolic function in the prenatal period. Copyright © 2017 ISUOG. Published by John Wiley & Sons Ltd.
Synthesis of citramalic acid from glycerol by metabolically engineered Escherichia coli
Authors: Wu Xianghao , Eiteman Mark A 
Published: July 2017

Abstract
Citramalic acid (citramalate) serves as a five-carbon precursor for the chemical synthesis of methacrylic acid. We compared citramalate and acetate accumulation from glycerol using Escherichia coli strains expressing a modified citramalate synthase gene cimA from Methanococcus jannaschii. These studies revealed that gltA coding citrate synthase, leuC coding 3-isopropylmalate dehydratase, and acetate pathway genes play important roles in elevating citramalate and minimizing acetate formation. Controlled 1.0 L batch experiments confirmed that deletions in all three acetate-production genes (poxB, ackA, and pta) were necessary to reduce acetate formation to less than 1 g/L during citramalate production from 30 g/L glycerol. Fed-batch processes using MEC568/pZE12-cimA (gltA leuC ackA-pta poxB) generated over 31 g/L citramalate and less than 2 g/L acetate from either purified or crude glycerol at yields exceeding 0.50 g citramalate/g glycerol in 132 h. These results hold promise for the viable formation of citramalate from unrefined glycerol.
Genetic diversity of Patellifolia patellaris from the Iberian Peninsula, a crop wild relative of cultivated beets
Authors: Frese Lothar , Bülow Lorenz , Nachtigall Marion , Rubio Teso María Luisa , Duarte Maria Cristina , Rey Elena , Iriondo Alegría José María 
Published: July 2017

AbstractThe genetic diversity ofPatellifolia patellarishas been investigated to generate information required for the organisation of a systematic genetic resources conservation action combining the best elements of the ex situ and in situ conservation concept. To this end, ten occurrences of the species were sampled on the Iberian Peninsula in Portugal and Spain. A total of 271 individuals was analysed using 24 microsatellite markers. The factorial analysis separated the material into two occurrences from Portugal, two occurrences sampled east of Gibraltar and six occurrences from the eastern Spanish coast. The pairwise genetic distance between occurrences and the complementary compositional differentiation among occurrences were calculated. The genetic distance values were used to construct an Unweighted Pair Group Method with Arithmetic Mean tree, which can be separated into four equidistant clusters. Two clusters are located in Portugal and two further clusters in Spain. The factorial analysis as well as the genetic distance and differentiation analysis indicate that the two occurrences from Portugal are clearly genetically different from the Spanish group of occurrences. Both occurrences have low population sizes and are therefore highly endangered. In situ conservation actions are urgently required for both occurrences. Further investigations are needed to organise better informed conservation actions forP. patellaris, namely to study genetic relationships between occurrences on the Spanish mainland and occurrences distributed on the Canary Islands, Madeira and Cape Verde Islands as well as in Morocco.
NGOization of Islamic Charity: Claiming Legitimacy in Changing Institutional Contexts
Authors: Borchgrevink Kaja 
Published: July 2017

AbstractIslamic welfare organizations are currently going through processes of ‘NGOization’. Drawing on qualitative data from Pakistan, Norway and the UK (2012–2015), this article examines how two Islamic welfare organizations which are embedded in Islamic political movements, become ‘Muslim NGOs’. The NGOization of Islamic charity signifies not only a change in organizational structure and legal status, but also more profound changes in organizational discourse and practice, and in the ways the organizations make claims to legitimacy. To claim legitimacy as providers of aid in changing institutional environments, the organizations draw on both religious and professional sources of authority. By analysing the NGOization of Islamic charity, the paper brings out the importance of normative frameworks in shaping organizational legitimacy and sheds light on the continued significance of both moral and transcendental aspects of the discourses, practices and identities of Muslim NGOs.
Impact of various issues on extending the useful life of a product through product recovery options
Authors: Mukherjee Kampan , Mondal Sandeep , Chakraborty Kaustov 
Published: July 2017

Abstract
Due to the growing consciousness towards environment and stringent governmental legislations, manufacturers are incorporating product recovery activities in their business processes. In product recovery process, used products are collected after their end-of-use from the customers and their retained usable values are recovered through value additive operations. The product recovery options not only reduce the disposal of wastes but also extend the useful life of product. In this paper, we try to identify various issues from literature review, which influence the extension of useful life of products through product recovery options. These issues are further classified into five major decision areas namely product design issues, operational issues, market related issues, governmental rules and legislations, and societal issues. The contextual relationships among these set of issues are studied by using Fuzzy Interpretive Structural Modelling (FISM), which reflects different levels of influence. Two case studies are highlighted here to compare the contextual relationships among these decision-making issues. The issues in the highest-level act as the prime enablers which trigger the extension of product life and help in formation of corporate strategies. The issues in the lower level generally act as operational issues.
Taurine supplementation to anti-seizure drugs as the promising approach to treat pharmacoresistant epilepsy: A pre-clinical study
Authors: Kumar Sandeep , Goel Rajesh 
Published: July 2017

AbstractBackground Pharmacoresistance leads to severe, irreversible disabilities and premature death in ∼30% cases of epilepsy despite adequate and appropriate treatment with available anti-seizure drugs (ASDs) without any underlying cause. In light of the large body of evidence which suggests the anti-seizure action of taurine in experimental animals and its wide safety margins in human, supplementation of this inhibitory amino-sulfonic acid to available ASDs seems promising to treat pharmacoresistant epilepsy.Methods We examined the anti-seizure effect of lamotrigine (15 mg/kg), levetiracetam (40 mg/kg), carbamazepine (40 mg/kg), phenytoin (35 mg/kg) & taurine (50, 100 & 200 mg/kg) in lamotrigine pre-treated pentylenetetrazole-kindled mice (LPK) which mimic core features of pharmacoresistant epilepsy, either alone ASDs or in combinations whereby three different doses of taurine were supplemented with tested ASDs.Results Both, the ASDs and the taurine were failed to suppress generalized tonic-clonic seizures in LPK mice. However, taurine supplementation clearly restored the anti-seizure effect of tested ASDs. Further neurochemical studies revealed that higher levels of taurine in the hippocampus and cerebral cortex restored the imbalance between major excitatory neurotransmitters glutamate & its inhibitory counterpart GABA.Conclusions These findings emphasize that supplementation of taurine with ASDs may be useful to treat pharmacoresistant epilepsy. Thus, further clinical validation is encouraged.
Acid-induced experimental muscle pain and hyperalgesia with single and repeated infusion in human forearm
Authors: Wang Kelun , Luo Yi , Asaki Toshiyuki , Graven-Nielsen Thomas , Cairns Brian E. , Arendt-Nielsen Thomas , Arendt-Nielsen Lars 
Published: July 2017

Abstract

Background and purpose
Acid has long been thought to play an important role in the pain process. Animal study showed that repeated acid stimulation induced central sensitization. The purpose of the study is to investigate muscle pain and hyperalgesia evoked byintramuscular infusion of saline at different pH levels, and to compare the effect of a single versus repeated acid infusions.

Methods
Twenty healthy subjects received infusions of buffered saline (pH 5.0, 6.0, and 7.4) into the brachioradialis muscle in a randomized order. Twelve of the subjects received repeated infusions. The subjects rated the pain intensity on visual analogue scale (VAS). Thermal pain sensitivity, and pressure pain threshold (PPT) were assessed in both arm before, during, immediately after, one hour after, and one day after the infusion. A McGill Pain Questionnaire and pain mapping were completed after each infusion.

Results
The pH 5 solution caused significantly higher pain and larger areas than pH 6.0 or 7.4. The local PPTs were significantly decreased (hyperalgesia) during and immediately after infusion of all three solutions. No significant differences were detected between the first and second infusion.

Conclusions
The intensity of acid-induced muscle pain is pH-dependent. All three solutions induced pressure hyperalgesia at the infusion site. Repeated infusions did not induce increased pain or prolonged hyperalgesia as compared with a single injection. Human intramuscular acidic saline infusion could not produce chronic pain model.

Implications
The acid-induced pain model may reflect the early stage responses to tissue injury of clinical conditions. Repeated intramuscular acidic saline injection model of prolonged hyperalgesia in rodents could not be translated into a human for modelling chronic musculoskeletal pain.
Canavangard, Udo Kasemets'sTrigon, and Marshall McLuhan: Graphic Notation in the Electronic Age
Authors: STRACHAN JEREMY 
Published: July 2017

AbstractComposer Udo Kasemets (1919–2014) emigrated to Canada in 1951 from Estonia following the Second World War, and during the 1960s undertook a number of initiatives to mobilize experimental music in Toronto. This article investigates Canavangard, Kasemets's publication series of graphic scores which appeared between 1967 and 1970. Influenced by Marshall McLuhan's spatial theory of media, Kasemets saw the transformative potential of non-standard notational practices to recalibrate the relationships between composer, performer, and listener. Kasemets's 1963 compositionTrigon, which was frequently performed by his ensemble during the decade, illuminates the connections between McLuhan and experimental music. In my analysis of the work, I argue thatTrigonmanifestly puts into performance many of the rhetorical strategies used by McLuhan to describe the immersive, intersensory environments of post-typographic media ecologies. Kasemets believed that abandoning standard notation would have extraordinary ramifications for musical practice going forward in the twentieth century, similar to how McLuhan saw the messianic power of electronic media to destabilize the typographic universe. Canavangard, as much more than a short-lived publication series of graphic scores, maps the convergences of music, culture, and technology in post-war Canada.