gebhart/patrepeval huggingface dataset:
N-Demethylation of morphine and structurally related compounds with chloroformate esters (1972)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTN-Demethylation of morphine and structurally related compounds with chloroformate estersM. M. Abdel-Monem and P. S. PortogheseCite this: J. Med. Chem. 1972, 15, 2, 208–210Publication Date (Print):February 1, 1972Publication History Published online1 May 2002Published inissue 1 February 1972https://pubs.acs.org/doi/10.1021/jm00272a025https://doi.org/10.1021/jm00272a025research-articleACS PublicationsRequest reuse permissionsArticle Views989Altmetric-Citations59LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
The effects of GH-releasing hormone/somatostatin on the 5'-promoter activity of the GH gene in vitro (2003)

The two hypothalamic hormones, GH-releasing hormone (GHRH) and somatostatin (SRIF), are known to regulate GH secretion. However, the effects of these hormones on GH gene expression are not completely clear, partly because of the lack of appropriate host cells maintaining the original characteristics of the somatotroph. Since MtT/S, a pure somatotroph cell line, has become available, the effects of GHRH and SRIF on GH gene transcription have been studied using a subclone of MtT/S (MtT/SGL), in which the GH gene 5'-promoter-luciferase fusion gene was stably incorporated. The expression of GHRH receptor and SRIF receptor subtypes was also studied by RT-PCR. The results showed that MtT/SGL cells intrinsically expressed the functional GHRH receptor and all of the SRIF receptor subtypes. The expression of GHRH receptor was markedly enhanced by glucocorticoid pretreatment and, in the presence of corticosterone and 3-isobutyl-1-methylxanthine, GHRH (at or above 100 pM) stimulated GH gene 5'-promoter activity in a dose-dependent manner. On the other hand, SRIF (100 nM) significantly antagonized the effect of GHRH, which was completely reversed by pretreatment with pertussis toxin (50 ng/ml). Taken together, the present data indicated that both GHRH and SRIF are involved in the transcriptional regulation of the GH gene, and that the effect of SRIF is mediated through pertussis toxin-sensitive G protein. The MtT/SGL cell line is a good in vitro model for studying the molecular mechanisms of GH gene transcription by GHRH and/or SRIF.
Radarsignaturen und ihre Veränderung durch Metamaterialien (2014)

Die Auswertung von Radarsignaturen anhand von 3-D-Modellen ist für Aufklärungsaufgaben ein wichtiges Hilfsmittel zur Objektanalyse. Für die Signaturreduktion können leichte und flexible Metamaterialien einen wesentlichen Beitrag leisten.
Bring Gait Lab to Everyday Life: Gait Analysis in Terms of Activities of Daily Living (2019)

With the development of the Internet of Things (IoT), wearable technologies have been proposed to measure gait parameters in everyday life. However, since both diseases and activities could influence gait patterns, clinicians cannot use the measured gait parameters for clinical applications without knowing the corresponding activities. To address this problem, a novel gait analysis method—“gait analysis in terms of activities of daily living (ADLs)”—was proposed based on a wearable Smart Insole system. Twenty six gait parameters were extracted to realize a systematic gait analysis. Novel activity recognition algorithms based on characteristics of human gait were proposed to recognize ADLs, including “sitting,” “standing,” “walking,” “running,” “ascend stairs,” and “descend stairs” with high accuracy and low computation load. To evaluate the performance of “gait analysis in terms of ADLs,” an experiment consisting of a sequence of different ADLs was designed to simulate the scenario of everyday life. In the result, gait parameters measured during different activities were automatically highlighted with different colors, which made it easy to see whether the gait pattern change was caused by activities or diseases. Besides, a refined gait analysis could be realized by individually extracting and analyzing the gait parameters of a specific activity. The results indicate that “gait analysis in terms of ADLs” is a feasible method to reach the aim of bringing gait lab to everyday life.
Overall Well-Focused Catadioptric Image Acquisition With Multifocal Images: A Model-Based Method (2012)

When a catadioptric imaging system suffers from limited depth of field, a single image can not capture all the objects with clear focus. To solve this problem, a set of multi-focal images can be used to extend the depth of field by fusing the best focused image regions to an overall well focused composite image. In this paper, we proposed a novel model based method that avoids the computational cost problem of previous extended-depth-of-field algorithms. Based on the special optical geometry properties of catadioptric systems, the proposed model describes the shapes of the best focused image regions in multi-focal images by a series of neighboring concentric annuluses. Then we proposed a method to estimate the model parameters. Based on this model, an overall well focused image is obtained by combining the best focused regions with a fast and reliable online operation. Experiments on catadioptric images of a variety of different scenes and camera settings verify the validity of the model and the robust performance of the proposed method.
Conversion of haloform to carbonate by iridium N-heterocyclic carbene complexes and silver(i) oxide (2019)

The reaction between haloform, the complexes [Cp*IrCl2(κC-MeNC3H2NCH2Ar)] (Ar = C6H3F2-2,6, C6H3F-2-Cl-6, C6H3Me2-2,6) and silver(i) oxide proceeded by carbon-halogen bond fission to yield the carbonate complexes [Cp*Ir(κ2O-CO3)(κC-MeNC3H2NCH2Ar)].
Histamine receptors as potential therapeutic targets to treat anxiety and depression (2005)

Abstract Increasing evidence supports a role for histamine in anxiety and depression. In most studies, histamine and stimulation of the histamine H 1 receptor (H 1 R) or blockade of the histamine H 2 receptor (H 2 R) increase measures of anxiety. In contrast, in most studies histamine reduces depression‐like activity, which might be related to effects of histamine on waking. These effects of histamine on anxiety and depression make histamine receptor ligands attractive therapeutic targets. As most studies assessing the potential of histamine receptor ligands on depression did not exclude potential effects of these ligands on locomotor activity, more studies are warranted to determine the exact role of histamine receptor subtypes in depression. The effects of histamine‐mediated signaling on anxiety and depression should also be considered in assessments of the potential of histamine H 3 receptor (H 3 R) ligands for conditions characterized by cognitive impairments as well as noncognitive behavioral impairments. Drug Dev. Res. 65:126–132, 2005. © 2005 Wiley‐Liss, Inc.
Elliptical-core, two-mode optical fibre sensors as vibration-mode filters (1991)

Ruggedised two-mode, elliptical-core fibre sensors are shown to be selective in sensing the different modal frequencies of vibration from a damped-damped beam. Sensor placement on a flexible structre is shown to be critical in the design of fibre sensors that measure an integral of strain over their entire sensing lengths. Experimental results confirm theoretical predictions and efficient vibration-mode selectivity is demonstrated.
The use of topical opioids to relieve pressure ulcer pain (2005)

This article provides an overview of the use of topical opioids to relieve pain associated with pressure ulcers in patients receiving palliative care. Morphine and diamorphine-infused gel have been used effectively to relieve pain and promote comfort in this group of patients.
A 94 GHz planar monopulse tracking receiver (1994)

This paper describes the design, fabrication and measurements of a 94 GHz integrated monopulse receiver with IF beam control. The receiver is integrated on a single chip, and is based on a 23 GHz local oscillator driving four separate phase-coherent 94 GHz subharmonic mixers. The resulting IF signals are takeoff-chip to a IF monopulse processor, which produces sum and difference monopulse patterns for the elevation and azimuth coordinates. Voltage-controlled phase-shifters in each of the IF channels allow the monopulse patterns to be electronically steered. All of the receiver circuits are realized using uniplanar coplanar-waveguide (CPW), slot lines and coplanar striplines (CPS). These features result in a compact, low-cost system suitable for tracking systems operating in poor visibility conditions, as well as in collision avoidance receivers for automotive applications. To our knowledge, this work represents the first demonstration of a fully integrated millimeter-wave subsystem to date.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Treatment with either high or low frequency TENS reduces the secondary hyperalgesia observed after injection of kaolin and carrageenan into the knee joint (1998)

For years, physical therapists have been utilizing a variety of modalities, including transcutaneous electrical nerve stimulation (TENS), in an attempt to manage pain associated with inflammation. However, the data on clinical effectiveness is conflicting and the neurophysiological mechanism of action is not known. The purpose of this study was to investigate the effects of high and low frequency TENS on the secondary hyperalgesia that occurs after joint inflammation. Secondary hyperalgesia is thought to reflect changes in central neurons and is thus a measure of activity of central neurons. This study utilized the kaolin and carrageenan model of knee joint inflammation and measured the effects of TENS treatment on paw withdrawal latency to radiant heat (secondary hyperalgesia), spontaneous pain behaviors and joint circumference. Either high (100 Hz) or low (4 Hz) frequency TENS was applied to the knee joint for 20 min after the development of hyperalgesia. Both high and low frequency TENS resulted in a reversal of the hyperalgesia immediately following treatment. The effects of high frequency TENS lasted through at least 24 h while those of low frequency TENS lasted through 12 h. There was no effect of TENS on spontaneous pain behaviors or joint swelling when compared to controls. Thus, TENS appears to be more effective in reducing referred pain (or secondary hyperalgesia) without affecting guarding or splinting of the affected limb. Thus, clinically, the choice to use TENS may depend on patient symptoms; specifically TENS should be effective in reducing referred or radiating pain.
Bacterial lyso-form lipoproteins are synthesized via an intramolecular acyl chain migration (2020)

All bacterial lipoproteins share a variably acylated N-terminal cysteine residue. Gram-negative bacterial lipoproteins are triacylated with a thioether-linked diacylglycerol moiety and an <i>N</i>-acyl chain. The latter is transferred from a membrane phospholipid donor to the α-amino terminus by the enzyme lipoprotein <i>N</i>-acyltransferase (Lnt), using an active-site cysteine thioester covalent intermediate. Many Gram-positive Firmicutes also have <i>N</i>-acylated lipoproteins, but the enzymes catalyzing <i>N</i>-acylation remain uncharacterized. The integral membrane protein Lit (<u>l</u>ipoprotein <u>i</u>ntramolecular <u>t</u>ransacylase) from the opportunistic nosocomial pathogen <i>Enterococcus faecalis</i> synthesizes a specific lysoform lipoprotein (<i>N</i>-acyl <i>S</i>-monoacylglycerol) chemotype by an unknown mechanism that helps this bacterium evade immune recognition by the Toll-like receptor 2 family complex. Here, we used a deuterium-labeled lipoprotein substrate with reconstituted Lit to investigate intramolecular acyl chain transfer. We observed that Lit transfers the <i>sn</i>-2 ester-linked lipid from the diacylglycerol moiety to the α-amino terminus without forming a covalent thioester intermediate. Utilizing Mut-Seq to analyze an alanine scan library of Lit alleles, we identified two stretches of functionally important amino acid residues containing two conserved histidines. Topology maps based on reporter fusion assays and cysteine accessibility placed both histidines in the extracellular half of the cytoplasmic membrane. We propose a general acid base-promoted catalytic mechanism, invoking direct nucleophilic attack by the substrate α-amino group on the <i>sn</i>-2 ester to form a cyclic tetrahedral intermediate that then collapses to produce lyso-lipoprotein. Lit is a unique example of an intramolecular transacylase differentiated from that catalyzed by Lnt, and provides insight into the heterogeneity of bacterial lipoprotein biosynthetic systems.
[Gliomas: the role of environmental risk factors and genetic predisposition]. (2005)

Exposure to ionising radiation is the only established risk factor for glioma. Although gliomas are looked upon as a non-heritable disease, physicians regularly see patients with affected relatives in practice. A few monogenetic tumour syndromes explain < 5% of all gliomas: neurofibromatosis type 1 and 2, Li-Fraumeni syndrome, tuberous sclerosis, Turcot syndrome, Gorlin syndrome, and the melanomaastrocytoma syndrome. Aggregation ofgliomas in families without these tumour syndromes also occurs. The overall familial pattern is generally atypical for hereditary cancers. Relatives are estimated to have a 2- to 9-fold increased risk. The occurrence ofgliomas in families can probably best be explained by a multifactorial model: environmental risk factors with a genetically determined susceptibility for these risk factors. The identity of the genetic variants leading to this predisposition remains to be determined. When there are indications of a hereditary tumour syndrome, additional diagnostic investigation is indicated.
Nanostructures from the self-assembly of α-helical peptide amphiphiles (2014)

Self-assembly of PAs composed of palmitic acid and several repeated heptad peptide sequences, C₁₅H₃₁CO-(IEEYTKK)(n)-NH₂ (n = 1-4, represented by PA1-PA4), was investigated systematically. The secondary structures of the PAs were characterized by CD. PA3 and PA4 (n = 3 and 4, respectively) showed an α-helical structure, whereas PA1 and PA2 (n = 1 and 2, respectively) did not display an α-helical conformations under the tested conditions. The morphology of the self-assembled peptides in aqueous medium was studied by transmission electron microscopy. As the number of heptad repeats in the PAs increased, the nanostructure of the self-assembled peptides changed from nanofibers to nanovesicles. Changes of the secondary structures and the self-assembly morphologies of PA3 and PA4 in aqueous medium with various cations were also studied. The critical micelle concentrations were determined using a pyrene fluorescence probe. In conclusion, this method may be used to design new peptide nanomaterials.
Biochemical and pharmacological properties of SR 27388, a dual antioxidant and PAF receptor antagonist. (1993)

SR 27388 (N-(2-dimethylaminoethyl)-N-(3-pyridinylmethyl[4-(3,5-di(tert- butyl)-4-hydroxylphenyl)thiazol-2-yl]amine) is a potent and competitive antagonist of the binding of [3H]PAF to its receptor on rabbit platelets exhibiting an equilibrium inhibition constant for PAF binding of 10.5 +/- 1.2 nM (n = 3). SR 27388 potently inhibited PAF-induced aggregation of rabbit platelets in vitro (IC50 = 65 +/- 12 nM) (n = 4). In this respect, SR 27388 was as potent as the triazolothienodiazepine WEB-2086 against PAF-induced aggregation of rabbit platelets and had no effect on the action of other platelet aggregating agents. SR 27388 prevented in a dose-dependent manner the formation of thiobarbituric acid reactive substances during membrane peroxidation (IC50 = 0.7 microM) and inhibited reduction of the stable 1,1-diphenyl-2-picrylhydrazyl radical, indicating that the antioxidant potency of SR 27388 was due to an efficient radical scavenging activity. SR 27388 displayed marked in vitro inhibition of zymosan-induced oxidative burst in human monuclear cells (IC50 = 3 microM). In vivo, SR 27388 protected mice from 100 micrograms/kg PAF-induced death with an ED50 value of 500 micrograms/kg, when given i.v., 5 min before PAF challenge or p.o. (ED50 = 800 micrograms/kg) when given 1 h before PAF administration. Similarly, i.v. or oral doses of SR 27388 afforded in mice complete protection against endotoxin-induced lethality (ED50 values were 250 micrograms/kg and 1.3 mg/kg, respectively). Neither BHT, vitamin E nor catechin exhibited significant protection against PAF- or endotoxin-induced death. In ovalbumin-presensitized rabbits, SR 27388 premixed with the allergen inhibited in a dose-dependent manner allergen-induced oedema formation in the skin (ED50 = 0.1 mumol/site). After an i.v. administration of 10 mg/kg, SR 27388 significantly protected mice against alloxan-induced diabetes. These results show that SR 27388 is a potent and orally active dual PAF receptor antagonist and antioxidant.
Abstract CT102: Efficacy and toxicity management of 19-28z CAR T cell therapy in B cell acute lymphoblastic leukemia (2014)

Abstract Chimeric antigen receptors (CARs) are artificial receptors for antigen that redirect antigen specificity, activate T cells and further enhance T cell function through their costimulatory component. Three groups, including our own, have reported objective tumor responses when infusing autologous T cells genetically modified with CD19-targeted CARs into patients with chronic lymphocytic leukemia (CLL), other indolent non-Hodgkin lymphomas (NHL) and, most dramatically in patients with relapsed or refractory B cell acute lymphoblastic leukemia (B-ALL). Here we report on 16 patients with relapsed or refractory B-ALL that we treated with autologous T cells expressing the 19-28z CAR specific to the CD19 antigen. The overall complete response rate was 88%, as assessed by morphological criteria and IgH deep sequencing. This allowed us to transition a majority of these patients to a standard of care allogeneic hematopoietic stem cell transplant (allo-SCT). This therapy was as effective in high-risk patients with Ph+ disease as in those with relapsed disease following prior allo-SCT. Through systematic analysis of clinical data and serum cytokine levels over the first 21 days following T cell infusion, we have defined diagnostic criteria for a severe cytokine release syndrome (sCRS), with the goal of better identifying the subset of patients who will likely require therapeutic intervention with corticosteroids or interleukin-6 receptor blockade to curb the CRS. Additionally, we found that serum C-reactive protein (CRP), a readily available laboratory study, can serve as a reliable indicator for the severity of the CRS and a road map for patient management at centers now contemplating the use of CAR T cell therapy. Based on these remarkably robust clinical results and the toxicity management algorithm we present here, we will soon open a multi-center Phase II clinical trial to further evaluate the efficacy of 19-28z CAR T cells and prospectively validate our proposed CRS monitoring and intervention guidelines in patients who are treated with CAR therapy. Citation Format: Michel Sadelain, Renier Brentjens, Marco Davila, Isabelle Riviere, Xiuyan Wang, Shirley Bartido, Jae Park, Diana Bouhassira, Kevin Curran, Stephen Chung, Jolanta Stefanski, Oriana Borquez-Ojeda, Sergio Giralt. Efficacy and toxicity management of 19-28z CAR T cell therapy in B cell acute lymphoblastic leukemia. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2014;74(19 Suppl):Abstract nr CT102. doi:10.1158/1538-7445.AM2014-CT102
Chemical Reaction Technology (2022)

The book discusses the sciences of operations, converting raw materials into desired products on an industrial scale by applying chemical transformations and other industrial technologies. Basics of chemical technology combining chemistry, physical transport, unit operations and chemical reactors are thoroughly prepared for an easy understanding.
Prediction of Polymer Glass Transition Temperatures Using a General Quantitative Structure−Property Relationship Treatment (1996)

A novel approach to the prediction of the physical properties of polymers is presented. A QSPR study, involving the use of a newly developed statistical package, CODESSA, is described for the Tg of a set of 22 low molecular weight polymers which gave a four-parameter equation with R2 = 0.928. The physical significance of the descriptors selected is discussed.
A Real-Time Hardware System for Digital Processing of Wide-Band Video Images (1976)

A high-fidelity video digitizer/processor extracts spatial and gray-scale information from high resolution dynamic video imagery. The 15-MHz bandwidth 60/s images(fields) are low pass filtered to minimize aliasing and digitized in real-time at 20 million samples pe second (MS/s), 9 bits/sample; sequential fields are transferred to memory, retrieved from memory after computer image processing, and reconstituted at up to 40 MS/s into 60 field/s video of 525, 875, or 1225 lines/frame (two interlaced fields). A/D and D/A converters are synchronized with memory by a high-speed interface, composed of a central data interchange (DI), and 8 rarially connected I/O ports. The DI connects the data paths of one or more ports, each communicating with one or more external devices. Separate 16-bit, 40 megawords/s, input and output data buses between each port and the DI allow data entry through any port to the DI and output from the DI through any port(s), even the same port from which the input originated. The A/D and D/A are served by a single port. Two other ports communicate with CDC 3500 and CDC 1700 computers. Yet another port controls up to two megawords of core/solid-state memory, of which 358K word may be accessed at the full data rate. Storage rates into existing memory of 40 MS/s are achieved for 16-32 ms.
Electromagnetic scattering from a dielectric-coated elliptic cylinder (1988)

An exact treatment using the boundary-value method for solving the problem of scattering of a line-source field or a plane wave by a perfectly conducting elliptic cylinder coated with a confocal dielectric elliptical shell is presented. For the line-source excitation the total field is calculated, while for the plane-wave excitation the echo width is obtained. A sample and interesting results for the backscattering echo width versus different geometrical parameters are obtained and presented. A set of design-type curves, which are useful for locating the maximum or minimum backscattering echo width, are also provided.
Treatment of Suicide Attempters With Bipolar Disorder: A Randomized Clinical Trial Comparing Lithium and Valproate in the Prevention of Suicidal Behavior (2011)

Despite the high frequency of suicide events during the study, this randomized controlled trial detected no difference between lithium and valproate in time to suicide attempt or suicide event in a sample of suicide attempters with bipolar disorder. However, smaller clinically significant differences between the two drugs were not ruled out.