gebhart/patrepeval huggingface dataset:
Multi-unit Controlled Release Systems of Nifedipine and Nifedipine:Pluronic® F-68 Solid Dispersions: Characterization of Release Mechanisms (2002)

Nifedipine (N) and nifedipine. Pluronic F-68 solid dispersion (SD) pellets were developed and characterizedfor drug release mechanisms from a multi-unit erosion matrix system for controlled release. Nifedipine was micronized using a jet mill. Solid dispersion with Pluronic F-68 was prepared by the fusion method. Nifedipine and SD were characterized by particle size analysis, solubility, differential scanning calorimetry (DSC), and x-ray diffraction (XRD) studies. Samples were subsequently processed into matrix pellets by extrusion/spheronization using Eudragit L 100-55 and Eudragit S 100 as release rate-controlling polymers. Drug release mechanisms from pellets were characterized by microscopy and mercury intrusion porosimetry; DSC and XRD studies indicated no polymorphic changes in N after micronization and also confirmed the formation of SD of N with Pluronic F-68. Pellets of N showed a 24-hr drug release profile following zero-order kinetics. Pellets of SD showed a 12-hr release profile followingfirst-order kinetics. Aqueous solubility of N after SD formation was found to be increased 10-fold. Due to increased solubility of N in SD, the drug release mechanism from the multi-unit erosion matrix changed from pure surface erosion to an erosion/diffusion mechanism, thereby altering the release rate and kinetics.
Binding of aminoglycoside antibiotics to helix 69 of 23S rRNA (2009)

Aminoglycosides antibiotics negate dissociation and recycling of the bacterial ribosome's subunits by binding to Helix 69 (H69) of 23S rRNA. Aminoglycoside binding to the chemically synthesized terminal domains of the E. coli and human H69 was detected and quantified using UV‐monitored thermal denaturation, circular dichroism spectrapolarimetry, and isothermal titration calorimetry. The unmodified E. coli H69 hairpin exhibited a significantly higher affinity for neomycin and tobramycin than for paromomycin, while the binding of streptomycin was too weak to assess. The three conserved pseudouridine modifications (Ψ1911, Ψ1915, Ψ1917) occurring in the loop of the E. coli H69 did not significantly effect the dissociation constant or stoichiometry for the binding of paromomycin. In contrast, the human 28S rRNA H69 had a considerably decreased affinity for the antibiotics. The higher affinity of the bacterial 23S rRNA H69 for aminoglycosides is an important validation of the antibiotic target. The higher affinity of the E. coli H69 for neomycin and tobramycin as compared to paromomycin and streptomycin indicates differences in the efficacy of the aminoglycosides as anti‐microbial agents.
Origin of the Preference for the Orbital Symmetry Forbidden Stereochemistry of the 1,5-Sigmatropic Shift of Substituted Norcaradienes (1999)

ADVERTISEMENT RETURN TO ISSUEPREVCommunicationNEXTADDITION / CORRECTIONThis article has been corrected. View the notice.Origin of the Preference for the Orbital Symmetry Forbidden Stereochemistry of the 1,5-Sigmatropic Shift of Substituted NorcaradienesAchim Kless, Maja Nendel, Sarah Wilsey, and K. N. HoukView Author Information Department of Chemistry and Biochemistry University of California Los Angeles, California 90095-1569 Cite this: J. Am. Chem. Soc. 1999, 121, 18, 4524–4525Publication Date (Web):April 27, 1999Publication History Received23 November 1998Published online27 April 1999Published inissue 1 May 1999https://pubs.acs.org/doi/10.1021/ja9840192https://doi.org/10.1021/ja9840192rapid-communicationACS PublicationsCopyright © 1999 American Chemical SocietyRequest reuse permissionsArticle Views602Altmetric-Citations46LEARN 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-AlertscloseSupporting Info (1)»Supporting Information Supporting Information SUBJECTS:Chemical structure,Potential energy,Rearrangement,Stereochemistry,Transition states Get e-Alerts
Development of Room Air Conditioner with Twin-Propeller Fans (2018)

In order to realize a significant energy conservation and comfort of room air conditioners, we have developed a new structure indoor unit which drastically reviewed the internal structure for the first time in about half a century. This indoor unit improves energy saving performance by changing the shape of the air passage matching the air flow through the indoor unit from the upper side to the lower side, changing to the fan shape suitable for the air passage, and efficient arrangement of the heat exchanger. We reduced the power consumption of the indoor unit by 31% and improved the APF by 13.3% compared with the previous year. In addition, we realized an improvement in comfort by controlling the airflow making full use of the features of the new fan shape.
TMI! Finetuned Models Leak Private Information from their Pretraining Data (2023)

Transfer learning has become an increasingly popular technique in machine learning as a way to leverage a pretrained model trained for one task to assist with building a finetuned model for a related task. This paradigm has been especially popular for $\textit{privacy}$ in machine learning, where the pretrained model is considered public, and only the data for finetuning is considered sensitive. However, there are reasons to believe that the data used for pretraining is still sensitive, making it essential to understand how much information the finetuned model leaks about the pretraining data. In this work we propose a new membership-inference threat model where the adversary only has access to the finetuned model and would like to infer the membership of the pretraining data. To realize this threat model, we implement a novel metaclassifier-based attack, $\textbf{TMI}$, that leverages the influence of memorized pretraining samples on predictions in the downstream task. We evaluate $\textbf{TMI}$ on both vision and natural language tasks across multiple transfer learning settings, including finetuning with differential privacy. Through our evaluation, we find that $\textbf{TMI}$ can successfully infer membership of pretraining examples using query access to the finetuned model. An open-source implementation of $\textbf{TMI}$ can be found on GitHub: https://github.com/johnmath/tmi-pets24.
A phase 3, double-blind, randomized study of pamiparib versus placebo as maintenance therapy in patients with inoperable, locally advanced, or metastatic gastric cancer that responded to platinum-based first-line chemotherapy - Trial in progress (2018)

Introduction: Gastric cancer is the fifth most common cancer and is the third leading cause of cancer deaths worldwide. A subset of gastric cancers exhibit platinum sensitivity and genomic instability that is characteristic of homologous recombination deficiency (HRD). Poly(ADP-ribose) polymerase proteins 1 and 2 (PARP1/2) are involved in DNA damage repair, and their inhibition is cytotoxic for cells with HRD. Pamiparib (previously known as BGB-290) is a selective PARP1/2 inhibitor that crosses the blood-brain barrier, has shown potent DNA–PARP trapping, and has demonstrated robust antitumor activity in preclinical models. In early phase clinical studies (NCT02361723; NCT03333915), pamiparib was generally well tolerated and showed promising antitumor activity. These studies also established 60 mg orally twice daily as the recommended pivotal dose. Methods: The purpose of this double-blind, placebo-controlled, randomized, multicenter Phase 3 study (NCT03427814) conducted in Asia, Australia, Europe, and North America is to compare the efficacy, safety, and tolerability of pamiparib with placebo as maintenance therapy in ∼540 patients with advanced gastric cancer who have responded to first-line, platinum-based chemotherapy. Patients who are ≤8 weeks after their last platinum dose of first-line chemotherapy will be randomized 1:1 to receive either pamiparib 60 mg twice daily or placebo in 28-day cycles. Patient randomization will be stratified by genomic loss of heterozygosity status (ie, high versus low), region, and ECOG status. Radiologic assessments will be centrally evaluated per RECIST every 8 weeks after first dose. Safety will be assessed on Day 1 of each cycle, and Day 15 of Cycles 1 and 2, and as needed. Blood samples will be collected at various time points to determine the pharmacokinetics of pamiparib in inoperable, locally advanced gastric cancer patients. The primary endpoint is progression-free survival; key secondary endpoints include safety/tolerability, overall survival, objective response rates, time and duration of response, and time to second subsequent treatment. Correlative biomarker analyses in tumor tissues and blood will be performed.
A novel nitroalkene vitamin E analogue inhibits the NLRP3 inflammasome and protects against inflammation and glucose intolerance triggered by obesity (2020)

Chronic metabolic diseases, like obesity, type II diabetes and atherosclerosis often involve a low-grade and sterile systemic inflammatory state, in which activation of the pro-inflammatory transcription factor NF-kB and the NLRP3 inflammasome play a major role. It is well established that genetic inhibition of the NLRP3 inflammasome ameliorates acute and chronic inflammation. Indeed, accumulating experimental evidences in murine models and also in humans suggest that inhibition of the NLRP3 inflammasome might be a suitable approach to tackle the deleterious effects of chronic metabolic diseases. In this work, we explored our previously synthesized nitroalkene-Trolox™ derivative named NATx0, as a non-conventional anti-inflammatory strategy to treat chronic inflammatory diseases, such as obesity-induced glucose intolerance. We found that NATx0 inhibited NF-kB nuclear translocation and pro-inflammatory gene expression in macrophages in vitro. In addition, treatment with NATx0 prevented NLRP3 inflammasome activation after LPS/ATP stimulation in macrophages in vitro. When tested acutely in vivo, NATx0 inhibited neutrophil recruitment in zebrafish larvae, and also diminished IL-1β production after LPS challenge in mice. Finally, when NATx0 was administered chronically to diet-induced obese mice, it decreased muscle tissue inflammation and glucose intolerance, leading to improved glucose homeostasis. In conclusion, we propose that this novel nitroalkene-Trolox derivative is a suitable tool to tackle acute and chronic inflammation in vitro and in vivo mainly due to inhibition of NF-kB/NLRP3 activation.
Enumeration and Analysis of DC-DC Converter Implementations Based on Piezoelectric Resonators (2019)

As demand for miniaturization in power electronics continues to rise, advances in achievable power density will eventually require new energy storage mechanisms whose fundamental size and efficiency limits are beyond those of traditional techniques. This motivates investigation into piezoelectric resonators (PRs), which are capable of very high power densities and efficiencies with emerging materials. PRs have been used in power conversion previously, but the realm of possible converter implementations using PRs has seen little exploration in the literature. In this work, we enumerate and downselect dc-dc converter topologies and switching sequences that utilize a PR as the only energy transfer component, and that provide low-loss "soft charging" of the PR capacitance for high efficiency. We present analysis methods for these converters' PR variable states, periodic steady state solutions, and energy transfer characteristics that offer insights for comparing topology and switching sequence options. These methods are then validated with an example PR-based converter implementation using LTspice simulations.
CuInSe/ZnS Core/Shell NIR Quantum Dots for Biomedical Imaging (2011)

CuInxSeY/ZnS core/shell quantum dots are synthesized with an emission peak in the near IR and a high quantum yield, suitable for biomedical imaging in the optical window. After lipid coating and transferring to water, the quantum dots show good stability, retain their high quantum yield, and have relatively small sizes to optimize circulation and clearance post-injection (P.I.).
Memory dependence prediction using store sets (1998)

For maximum performance, an out-of-order processor must issue load instructions as early as possible, while avoiding memory-order violations with prior store instructions that write to the same memory location. One approach is to use memory dependence prediction to identify the stores upon which a load depends, and communicate that information to the instruction scheduler. We designate the set of stores upon which each load has depended as the load's "store set". The processor can discover and use a load's store set to accurately predict the earliest time the load can safely execute. We show that store sets accurately predict memory dependencies in the context of large instruction window, superscalar machines, and allow for near-optimal performance compared to an instruction scheduler with perfect knowledge of memory dependencies. In addition, we explore the implementation aspects of store sets, and describe a low cost implementation that achieves nearly optimal performance.
Preferential CO oxidation in a H2-rich stream promoted by ReOx species attached to Pt metal particles (2009)

Clusters of ReO(x) are formed and attached to Pt metal particles during H(2) reduction treatment on Pt-ReO(x)/SiO(2), and the synergy between Pt metal surface and neighboring ReO(x) clusters gives high catalytic performance in the preferential CO oxidation in the presence of H(2)O and CO(2) as more realistic reaction conditions at low reaction temperature.
Electrical Breakdown and Recovery of Water and Propylene Carbonate (2005)

Polar liquids, especially water, offer the advantages of high permittivity, a high dielectric strength and a fast dielectric recovery. These benefits make them appealing dielectrics for use in high-energy storage systems and as high-power switching media. In certain applications, however, the use of water is limited by its relatively high freezing point of 0degC and low boiling point 100degC. In comparison, propylene carbonate (C <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">4</sup> H <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">6</sup> O <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sup> ) has a freezing temperature of -55degC and boiling point of 243degC in addition to its high permittivity of 65. The dielectric strength was found to be 2.3 MV/cm, slightly higher than that of water tested under the same conditions. As an alternative to water in high repetition rate systems we studied the dielectric recovery of propylene carbonate after breakdown. We found the recovery time to be more than one order of magnitude longer than for water. Moreover, the breakdown in propylene carbonate gives rise to a polymer formation in the liquid.
Cavity Stabilized X-Band Gunn Oscillator (1970)

The design and resultant experimental investigation of a pulling mechanism for a highly stable X-band Gunn oscillator, stabilized by a high Q TE/sub 011/-mode reflection cavity, are described. The oscillator shows a temperature coefficient of less than -7 x 10/sup -7/ / /spl deg/C,a low FM noise of 8 Hz per 1-kHz BW at 100 kHz from the carrier, and a wide-band mechanical-tuning capability of several hundred megahertz. In addition, experimental results concerning the hysteresis phenomena of oscillating frequencies, power, FM-noise versus cavity-pulling frequencies, and bias voltages are described.
P-glycoprotein expression and chemosensitivity in highly purified fresh human gastrointestinal cancer cells. (1999)

The chemotherapeutic management of patients with colorectal cancer might be more effective if we can circumvent the effect of P-glycoprotein.
High-performance solution processed oxide TFT with aluminum oxide gate dielectric fabricated by a sol–gel method (2011)

We have studied the fabrication of solution processed aluminum-oxide (AlOx) gate dielectric at the maximum process temperature of 300 °C for a solution based zinc-tin-oxide (ZTO) thin-film-transistor (TFT). An AlOx layer was spin-coated from a solution of aluminum chloride (AlCl3) and then annealed at 300 °C for 1 h. The breakdown electrical field and leakage current density of the AlOx were found to be ∼4 MV cm−1 and 63 μA cm−2 at 1 MV cm−1, respectively. The ZTO layer was prepared by spin-coating or inkjet printing as an active layer of the TFT with AlOx gate dielectric and then annealed at 300 °C for 1 h. The TFT made using spin coating exhibited the field-effect mobility of 33 cm2 V−1s−1 in the saturation region, a gate swing of 96 mV dec.−1 and a threshold voltage of ∼1.2 V and the inkjet printed TFT showed a field-effect mobility of 24 cm2 V−1s−1.
279 Regression of phrenic nerve injury after AF ablation (2005)

values between not inducible MD1 and VANH patients p=NS), while a difference was observed between inducible MD1 and VANH patients (2.324-4% and -2.94-1.8%respectively, p<0.001).Conclusions: our data suggest a dysfunction of the nervous autonomic system, assessed by HRT analysis, in MD1 respect to VANH patients, more evident in inducible MD1 patients.Therefore TO seems an useful non invasive risk predictor of sustained ventricular arrhythmias induced at EPS in MD 1 patients.
Asymmetric Optical Second-Harmonic Generation from ChiralG-Shaped Gold Nanostructures (2010)

We present a new electromagnetic phenomenon-the asymmetric second-harmonic generation from planar chiral structures. The effect consists in distinguishing the handedness of a chiral material by rotating the sample in an experiment involving solely linearly polarized light. This phenomenon originates in the surface plasmon resonance of chiral gold nanostructures, where homodyne interference of anisotropic and chiral electric and/or magnetic multipoles appears to play an important role.
Experimental study of multiple scattering in anisotropic titanium alloys (2017)

Ultrasonic testing of jet engine titanium alloys is of high importance for the aircraft manufacturing industry. The quality of ultrasonic non-destructive testing is severely impacted by the titanium complex microstructure. These alloys have been extensively studied and single scattering models are now well known and implemented in ultrasonic propagation simulators. In addition, titanium billets and forged parts have been known to exhibit a highly anisotropic microstructure. We studied ultrasonic wave scattering in Ti17 forged disk, through statistical analysis of the backscattered noise generated by the microstructure. More specifically, we focused on the quantification of multiple scattering relative to single scattering in the backscattered wave. To that end, we used the full matrix capture acquisition with a linear transducer array. Two phenomena were used to quantify the proportion of single scattering with respect to multiple scattering. The first is the coherent backscattering effect, used as a binary indicator of multiple scattering. The second is a repurposed version of the multiple scattering filter, recently developed on random rod forest and applied on Inconel alloys. With these methods, significant level of multiple scattering was consistently measured in Ti17 forged disks, showing that ultrasonic testing could be enhanced by filtering the multiple scattering contribution.
Nausea and vomiting in gastroparesis: similarities and differences in idiopathic and diabetic gastroparesis (2016)

Nausea is present in essentially all patients with gastroparesis irrespective of cause and associated with decreased quality of life. In contrast, vomiting was more prevalent, more severe, and occurred more often in DG than IG. Thus, characteristics of vomiting differ in IG vs DG.
Supplementary Figure 1 from Chk2 Phosphorylation of Survivin-ΔEx3 Contributes to a DNA Damage–Sensing Checkpoint in Cancer (2023)

&lt;p&gt;PDF file - 27K, GPL5188 platform probeset examined in this study. A. Relationship between all probeset expression profiles. B. Hierarchical clustering of expression profiles of probesets retained for analysis.&lt;/p&gt;
IL-1 is an autocrine growth factor for T cell clones. (1988)

Abstract Activation of Th lymphocytes requires that Ag be presented on the surface of accessory cells displaying Ia Ag. A number of studies have concluded that the T cell also requires IL-1 from accessory cells. However, we recently reported that one murine T cell clone (D10.G4.1) produced its own IL-1-like activity after encountering APC (9). In this report, we demonstrate that 1) IL-1 production is a common property of murine T cell clones, 2) T cell IL-1 activity is blocked by anti-IL-1-alpha antiserum, 3) IL-1-alpha mRNA can be directly visualized in individual cloned T cells using in situ hybridization techniques, and 4) IL-1 appears to serve an autocrine role in the activation of T cell clones inasmuch as anti-IL-1-alpha antiserum blocks cell proliferation when the T cell is the only IL-1 source.
Z944, a Novel Selective T-Type Calcium Channel Antagonist Delays the Progression of Seizures in the Amygdala Kindling Model (2015)

Temporal lobe epilepsy (TLE) is the most common form of drug resistant epilepsy. Current treatment is symptomatic, suppressing seizures, but has no disease modifying effect on epileptogenesis. We examined the effects of Z944, a potent T-type calcium channel antagonist, as an anti-seizure agent and against the progression of kindling in the amygdala kindling model of TLE. The anti-seizure efficacy of Z944 (5mg/kg, 10mg/kg, 30mg/kg and 100mg/kg) was assessed in fully kindled rats (5 class V seizures) as compared to vehicle, ethosuximide (ETX, 100mg/kg) and carbamazepine (30mg/kg). Each animal received the seven treatments in a randomised manner. Seizure class and duration elicited by six post-drug stimulations was determined. To investigate for effects in delaying the progression of kindling, naive animals received Z944 (30mg/kg), ETX (100mg/kg) or vehicle 30-minutes prior to each kindling stimulation up to a maximum of 30 stimulations, with seizure class and duration recorded after each stimulation. At the completion of drug treatment, CaV3.1, CaV3.2 and CaV3.3 mRNA expression levels were assessed in the hippocampus and amygdala using qPCR. Z944 was not effective at suppressing seizures in fully kindled rats compared to vehicle. Animals receiving Z944 required significantly more stimulations to evoke a class III (p<0.05), IV (p<0.01) or V (p<0.0001) seizure, and to reach a fully kindled state (p<0.01), than animals receiving vehicle. There was no significant difference in the mRNA expression of the T-type Ca2+ channels in the hippocampus or amygdala. Our results show that selectively targeting T-type Ca2+ channels with Z944 inhibits the progression of amygdala kindling. This could be a potential for a new therapeutic intervention to mitigate the development and progression of epilepsy.