gebhart/patrepeval huggingface dataset:
Activation and Desensitization of Hippocampal Kainate Receptors (1997)

We have used whole-cell recordings and rapid agonist applications to characterize the physiological properties of kainate receptors expressed by rat hippocampal neurons in dissociated cell culture. Activation of NMDA and AMPA receptors was prevented by inclusion of the noncompetitive antagonists MK-801 (2 microM) and GYKI 53655 (100 microM), respectively. In the presence of these inhibitors, both kainate (EC50 = 23 microM) and glutamate (EC50 = 310 microM) evoked desensitizing currents. Maximal peak currents for kainate with GYKI 53655 were 15 +/- 3% as large as in control solutions without GYKI. In contrast to currents mediated by AMPA receptors, kainate currents recorded in GYKI were blocked potently by lanthanum (IC50 = 2 microM) and were desensitized by 1 microM 2S,4R-4-methylglutamate (SYM 2081). Coapplication of either 5 microM AMPA or 500 microM aspartate had little effect on responses to kainate, although AMPA alone elicited current at 1 mM. In most cells, the currents evoked by kainate, glutamate, and SYM 2081 varied linearly with membrane potential and reversed near 0 mV. Kainate elicited substantial current at steady state (approximately 30% of peak), whereas responses to glutamate and SYM 2081 desensitized almost completely within 0.2-2 sec. Inhibition produced by a 10 sec desensitizing prepulse was half-maximal at 0.22 microM for SYM 2081 and 13 microM for glutamate. Recovery from desensitization to kainate and glutamate was >80% complete within 60 sec but was three- to fourfold slower after exposure to SYM 2081. Exposure to Concanavalin A blocked desensitization of the currents but also reduced the peak current amplitudes. Collectively, these results confirm that kainate-preferring receptors underlie the currents evoked by kainate, glutamate, or SYM-2081 in the presence of GYKI 53655; they are not mediated by electrogenic transport or by AMPA-preferring receptors that are insensitive to GYKI. In contrast to previous work on embryonic hippocampal neurons, our results show that the properties of kainate receptors expressed by cells from older animals are distinct from those displayed by homomeric assemblies of the GluR6 subunit.
Through-space amide activation of carbon-hydrogen bonds in triangulanes (1993)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTThrough-space amide activation of carbon-hydrogen bonds in triangulanesPhilip E. Eaton and Kirill A. LukinCite this: J. Am. Chem. Soc. 1993, 115, 24, 11370–11375Publication Date (Print):December 1, 1993Publication History Published online1 May 2002Published inissue 1 December 1993https://pubs.acs.org/doi/10.1021/ja00077a041https://doi.org/10.1021/ja00077a041research-articleACS PublicationsRequest reuse permissionsArticle Views366Altmetric-Citations36LEARN 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
Synthesis of 1,4,5,6‐tetrahydropyrazolo[3,4‐d]pyrido[3,2‐b]azepine (2000)

Abstract The synthesis of 7,8‐dihydro‐5(6 H )‐quinolinone ( 3 ) from commercially available 3‐amino‐2‐cyclohexen‐1‐one ( 1 ) and 3‐(dimethylamino)acrolein ( 4 ) in 23% yield avoids the preparation of propynal ( 2 ). Conversion of 5‐(4‐methylphenylsulfonyl)‐6,7,8,9‐tetrahydro‐5 H ‐pyrido[3,2‐ b ]azepine ( 12 ) to 6‐(4‐methylphenylsulfonyl)‐1,4,5,6‐tetrahydropyrazolo[3,4‐ d ]pyrido[3,2‐ b ]azepine ( 24 ) is described. Removal of the N ‐(4‐methylphenylsulfonyl) group with 40% sulfuric acid in acetic acid gave the tricyclic azepine 26. Application of a similar series of reactions to 5‐(4‐nitrobenzoyl)‐6,7,8,9‐tetrahydro‐5 H ‐pyrido[3,2‐ b ]‐azepine ( 13 ) afforded 6‐(4‐nitrobenzoyl)‐1,4,5,6‐tetrahydropyrazolo[3,4‐ d ]pyrido[3,2‐ b ]azepine ( 25 ).
Rapid mobilization of hematopoietic progenitor cells in rhesus monkeys by a single intravenous injection of interleukin-8 (1996)

Interleukin-8 (IL-8) is a chemoattractant cytokine involved in chemotaxis and activation of neutrophils. Because in vivo administration of IL-8 induces mobilization of hematopoietic stem cells in mice, we assessed the mobilizing properties of IL-8 in rhesus monkeys. Recombinant human IL-8 was administered as a single intravenous injection at doses of 10, 30, and 100 micrograms/kg to rhesus monkeys (age, 2 to 3 years; weight, 2.5 to 4.5 kg). Venous blood samples were obtained at time intervals ranging from 1 to 480 minutes after IL-8 administration. Cell counts, colony-forming unit-Mix assays, and fluorescence-activated cell sorter analysis were performed. Plasma was harvested to assess IL-8 levels. A time-controlled bolus intravenous injection of 100 micrograms IL-8 per kilogram of body weight resulted in peak IL-8 plasma levels up to 5 micrograms/mL. The calculated half-time life of free IL-8 was 9.9 +/- 2.2 minutes. IL-8 injection resulted in instant neutropenia that was due to pulmonary sequestration, as shown using 99mTc-labeled leukocytes. Within 30 minutes after IL-8 injection, neutrophilia developed with counts up to 10-fold greater than baseline levels. The numbers of hematopoietic progenitor cells (HPCs) increased from 45 +/- 48/mL to 1,382 +/- 599/mL of blood at 30 minutes after injection of 100 micrograms IL-8 per kilogram of bodyweight (mean +/- SD, n = 8). Individual animals showed 10- to 100-fold increase in numbers of circulating HPCs that returned to almost pretreatment values (92 +/- 52 CFU/mL) at 240 minutes after the injection of IL-8. Immunophenotyping showed no significant changes in lymphocyte (sub)populations. A second bolus injection of IL-8 with an interval of 72 hours resulted in similar numbers of mobilized stem cells as observed after the first injection, showing that no tachyphylaxis had occurred. We conclude that IL-8 induces mobilization of HPCs from the bone marrow of rhesus monkeys in a rapid and reproducible fashion. Therefore, IL-8 may be a potentially useful cytokine in the setting of blood stem cell transplantation.
10 Gbps millimeter-wave OFDM experimental system with iterative phase noise compensation (2013)

This paper presents a 10 Gbps millimeter wave OFDM experimental system using a highly efficient modulation and coding scheme where iterative phase noise compensation can drastically alleviate performance degradation due to phase noise. 60 GHz frequency synthesizer in a silicon RF-CMOS IC suffers from relatively large phase noise, which severely degrades the performance of the 10 Gbps OFDM using 64QAM and LDPC code with coding rate of 14/15. In order to alleviate this impairment, the experimental system applies combination of decision-directed phase noise compensation (DD-PNC), decision-directed channel estimation (DDCE) and packet interleaving (P-IL) to OFDM reception processing. The sophisticated combination of iterative processing provides a synergistic effect on coping with the influence of the phase noise by exploiting outputs of the LDPC decoder. Experimental results of the 10 Gbps OFDM with 60 GHz cable connection demonstrate that the combination can achieve 10 Gbps throughput at SNR of 25.8 dB when the phase noise level is -89 dBc/Hz at 1 MHz offset.
Antitumor activity of tumor necrosis factor-alpha conjugated with polyvinylpyrrolidone on solid tumors in mice. (2000)

We attempted the development of a novel polymer conjugation to further improve the therapeutic potency of antitumor cytokines compared with PEGylation for clinical application. Compared with native tumor necrosis factor (TNF)-alpha in vitro, specific bioactivities of polyvinyl-pyrrolidone (PVP)-modified TNF-alphas (PVP-TNF-alphas) were decreased by increasing the degree of PVP attachment. PVP-TNF-alpha fraction 3, Mr 101,000, had the most effective antitumor activity of the various PVP-TNF-alphas in vivo. PVP-TNF-alpha fraction 3 had >200-fold higher antitumor effect than native TNF-alpha, and the antitumor activity of PVP-TNF-alpha fraction 3 was >2-fold higher than that of MPEG-TNF-alpha (Mr 108,000), which had the highest antitumor activity among the polyethylene glycol (PEG)-conjugated TNF-alphas. Additionally, a high dose of native TNF-alpha induced toxic side effects such as body weight reduction, piloerection. and tissue inflammation, whereas no side effects were observed after i.v. administration of PVP-TNF-alpha fraction 3. The plasma half-life of PVP-TNF-alpha fraction 3 (360 min) was about 80- and 3-fold longer than those of native TNF-alpha (4.6 mm) and MPEG-TNF-alpha (122 min), respectively. The mechanism of increased antitumor effect in vivo caused the prolongation of plasma half-life and increase in stability. These results suggested that PVP is a useful polymeric modifier for bioconjugation of TNF-alpha to increase its antitumor potency, and multifunctionally bioconjugated TNF-alpha may be a potentiated antitumor agent for clinical use.
Semiconductor materials and devices (1989)

This chapter, which brings together for the first time an account of GEC&apos;s research and development on semiconductor materials and devices from 1940 until 1984, is based on contributions from a number of colleagues including, particularly, Clive Foxell (now Managing Director for Engineering and Procurement in British Telecom), Ralph Knott (now Chief Engineer at Marconi Electronic Devices, Lincoln), and Jack Lamming and Frank Hilsden who are still at the Research Laboratories. Consideration was given to splitting the Chapter into sections on, for exam ple, diodes (microwave and power), transistors (signal and power), thyristors, and materials. There have been, however, so many interrelations between the technologies for various devices, and between developments in materials and devices, that it has proved better to write a single account which is mainly chronological. The narrative attempts to bring together related developments and, as a result, it is sometimes necessary to depart from strict chronological order. It is hoped that an understandable account is nevertheless given of individual developments over the years, against a background of broad ad vances in semiconductor technology and organisational changes which inevit ably influenced the programme from time to time.
Economic evaluation of sacral neuromodulation in overactive bladder: A Canadian perspective (2015)

SNM is a cost-effective treatment option to manage patients with refractory OAB when compared to either BonT-A or OMT. From a Canadian payers' perspective, SNM may be considered a first-line treatment option in management of patients with OAB with superior long-term outcomes. Similar to all economic analysis, this study has limitations which are based on the assumptions of the used model.
Two splicing variants of a new inhibitor of apoptosis gene with different biological properties and tissue distribution pattern (2001)

Using homology searches, we identified a novel human inhibitor of apoptosis (IAP) gene. This gene has two splicing variants that contain open reading frames of 298 and 280 amino acids and both contained a single copy of baculovirus IAP repeat (BIR) and RING domain. We refer here to the longer and shorter variants as Livin alpha and beta, respectively. Semiquantitative reverse transcriptase-polymerase chain reaction demonstrated a tissue-specific and non-correlated expression pattern in both adult and fetal tissues. Both mRNA variants were detected in various transformed cell lines. Despite their very close similarity, the two isoforms have different antiapoptotic properties. Both isoforms have a significant antiapoptotic activity in the Jurkat T cell line after triggering apoptosis via tumor necrosis factor and CD95 receptors. The Livin alpha but not beta protects cells from apoptosis induced by staurosporine, but in contrast, apoptosis initiated by etoposide was blocked only by the beta isoform. This difference in biological activities may indicate the presence of critical amino acids outside the BIR and RING domains. These functional and tissue distribution differences of Livin alpha and beta suggest that Livin may play a complex role in the regulation of apoptosis.
Home media atomizer: remote sharing of home content - without semi-trusted proxies (2008)

This paper proposes a solution that allows home hosted content, located on home PCs or UPnP media servers, to be offered to remote clients, for consumption. The system is based on a proxy residing on the home network that exports the multimedia content to a Web syndication feed following the Atom protocol, which is then accessed from compatible remote clients. A prototype of the system was built, with the proxy functionality implemented on a home PC and the remote clients running on mobile phones. Special attention has been paid to the social aspects of content sharing, for allowing the home owner to also invite other external users to remotely access specific, home-based media containers, with very simple and secure device configuration.
Derivation of 3D coordinate templates for searching structural databases: Application to ser‐His‐Asp catalytic triads in the serine proteinases and lipases (1996)

It is well established that sequence templates (e.g., PROSITE) and databases are powerful tools for identifying biological function and tertiary structure for an unknown protein sequence. Here we describe a method for automatically deriving 3D templates from the protein structures deposited in the Brookhaven Protein Data Bank. As an example, we describe a template derived for the Ser-His-Asp catalytic triad found in the serine proteases and triacylglycerol lipases. We find that the resultant template provides a highly selective tool for automatically differentiating between catalytic and noncatalytic Ser-His-Asp associations. When applied to nonproteolytic proteins, the template picks out two "non-esterase" catalytic triads that may be of biological relevance. This suggests that the development of databases of 3D templates, such as those that currently exist for protein sequence templates, will help identify the functions of new protein structures as they are determined and pinpoint their functionally important regions.
Interleukin-11 attenuates pulmonary inflammation and vasomotor dysfunction in endotoxin-induced lung injury (1999)

Interleukin (IL)-11, like other members of the gp130 receptor class, possesses anti-inflammatory properties. We hypothesized that IL-11 pretreatment would attenuate endotoxin [lipopolysaccharide (LPS)]-induced lung inflammation and diminish injury to endothelium-dependent and -independent mechanisms of pulmonary vasorelaxation that require cGMP in Sprague-Dawley rats. LPS (20 mg/kg ip) increased lung tumor necrosis factor (TNF)-alpha compared with the saline control (0.7 +/- 0.15 ng/g lung wet wt for control vs. 3.5 +/- 0.09 ng/g lung wet wt for LPS; P < 0.05). IL-11 (200 mg/kg ip) injected 10 min before LPS administration attenuated the LPS-induced lung TNF-alpha levels (1.6 +/- 0.91 ng/g lung wet wt; P < 0.05 vs. LPS). IL-11 also diminished LPS-induced lung neutrophil sequestration as assessed by myeloperoxidase units (2.1 +/- 0.25 U/g lung wet wt for saline and 15.6 +/- 2.02 U/g lung wet wt for LPS vs. 7.07 +/- 1.65 U/g lung wet wt for LPS plus IL-11; P < 0.05). Similarly, TNF-alpha binding protein (175 mg/kg) attenuated LPS-induced myeloperoxidase activity (6.04 +/- 0.14 U/g lung wet wt; P < 0.05). Both IL-11 and TNF-alpha binding protein similarly attenuated LPS-induced endothelium-dependent vasomotor dysfunction with improved relaxation responses to 10(-7) and 10(-6) M acetylcholine and A-23187 in phenylephrine-preconstricted isolated pulmonary artery rings (P < 0.05 vs. LPS). Endothelium-independent relaxation responses to sodium nitroprusside were also improved after LPS at 10(-6) M (P < 0.05 vs. LPS). Moreover, IL-11 decreased endotoxin-induced mortality in CF1 mice from 90 to 50% (P </= 0.05 vs. LPS). Therefore, IL-11 prevents LPS-induced lung TNF-alpha production, neutrophil sequestration, and pulmonary vasomotor dysfunction. We conclude that IL-11 possesses anti-inflammatory activity that protects against LPS-induced lung injury and lethality.
The natural product hymenialdisine inhibits interleukin-8 production in U937 cells by inhibition of nuclear factor-kappaB. (1997)

The nuclear factor-kappaB (NF-kappaB) family of transcription factors have been implicated in the inducible expression of genes involved in inflammatory and immune responses. As such, a specific inhibitor of NF-kappaB would be a useful therapeutic agent in a variety of inflammatory disorders. The marine natural product hymenialdisine was evaluated as an inhibitor of NF-kappaB in U937 cells. U937 cells were transfected with either a luciferase reporter plasmid containing the human immunodeficiency virus long terminal repeat or the interleukin-8 (IL-8) core promoter, both of which are activated by NF-kappaB. Hymenialdisine caused a concentration-dependent decrease in luciferase production from both reporters when the cells were stimulated with tumor necrosis factor-alpha, lipopolysaccharide or phorbol myristate acetate. An electrophoretic mobility shift assay confirmed its activity by inhibiting DNA binding of NF-kappaB. Hymenialdisine was shown to be a selective inhibitor of NF-kappaB in that it had no effect on the binding of other transcription factors to their DNA concensus motifs; these included activator protein-1, CCAAT/enhancer binding protein and Sp1. Functional studies showed hymenialdisine to be an inhibitor of IL-8 production and IL-8 mRNA formation in the U937 cell. Investigation into the mechanism of action of hymenialdisine showed that it was not due to inhibition of protein kinase C because the selective protein kinase C inhibitor RO 32-0432 was inactive against tumor necrosis factor-alpha-stimulated luciferase and IL-8 production. The compound also had no effect on IkappaB alpha or IkappaB beta phosphorylation and degradation. Thus, hymenialdisine is a potent inhibitor of NF-kappaB and IL-8 production in U937 cells.
Cablemodem standards for advanced quality of service deployments (2003)

The DOCSIS standard has provided a basis for the cablemodem market to take off around interoperable, multi-vendor products. The evolution of this standard to include enhanced quality of service (QoS) and enhanced physical layers affords opportunities to deploy QoS intensive applications such as voice over IP, T1 circuit replacement, interactive gaming, multimedia enhanced services and video conferencing as well as address European deployment requirements. This paper addresses the DOCSIS 1.0, 1.1 and the new 1.2 standard and its evolving features, how it compares to the DVB-RC European proposal, and what QoS services and performance levels can be obtained. Detailed analysis of mixed QoS scenarios including multi-tiered committed information rate IP service and voice over IP are presented.
Peroxide-initiated addition of some polyfluorochloro- and polyfluorobromoalkanes to some hydrocarbon olefins (1969)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTPeroxide-initiated addition of some polyfluorochloro- and polyfluorobromoalkanes to some hydrocarbon olefinsPaul Tarrant and J. P. TandonCite this: J. Org. Chem. 1969, 34, 4, 864–869Publication Date (Print):April 1, 1969Publication History Published online1 May 2002Published inissue 1 April 1969https://pubs.acs.org/doi/10.1021/jo01256a019https://doi.org/10.1021/jo01256a019research-articleACS PublicationsRequest reuse permissionsArticle Views215Altmetric-Citations16LEARN 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
Oral Fluoride Measurements for Estimation of the Anti-caries Efficacy of Fluoride Treatments (1992)

The aims of this work were (a) to assess the oral bioavailability of fluoride delivered from dentifrices and (b) to test for a possible link between the results and clinical data obtained with the same dentifrices. Oral fluoride concentrations were measured in samples of saliva and plaque taken from seven subjects, after use of dentifrices which contained 0, 1000, 1500, and 2500 micrograms F/g as sodium monofluorophosphate. Salivary fluoride in samples obtained within the first few hours after a single dentifrice application, or up to 20 h after four weeks' daily use, increased with increasing F content of the dentifrice. For example, the mean zero-time intercepts of the second phase of salivary fluoride clearance curves for the above dentifrices were 0.46, 1.48, 1.88, and 3.03 mumol F/L, respectively. Plaque fluoride measured after four weeks' daily use of the dentifrices exhibited similar dose-response behavior. Linear regression analysis showed these trends to be statistically significant for both saliva (p less than 0.001) and plaque (p less than 0.025). Mean saliva and plaque fluoride concentrations were inversely associated with mean three-year caries increments for the three fluoride-containing dentifrices obtained in a recent clinical trial: DMFS scores 6.80, 6.33, and 5.71, respectively (Stephen et al., 1988). This suggests that oral fluoride measurements are a valuable in vivo method for the evaluation of the potential anti-caries efficacy of fluoride-containing dental products.
The effect of acute renal failure on mortality. A cohort analysis. (1996)

The high mortality rate in acute renal failure is not explained by the underlying conditions alone. Renal failure appears to increase the risk of developing severe nonrenal complications that lead to death and should not be regarded as a treatable complication of serious illness.