gebhart/patrepeval huggingface dataset:
In vivo binding of [<sup>125</sup>I] RTI‐55 to dopamine transporters: Pharmacology and regional distribution with autoradiography (1992)

Previous studies have demonstrated that para-substituted WIN 35,065-2 analogs of cocaine show high binding affinity for dopamine uptake sites both in vitro and in vivo, and inhibit DA uptake in vitro. These analogs also produce potent cocaine-like behavioral effects in various procedures. The purpose of the present studies was to evaluate the iodinated WIN 35,065-2 analog [125I]RTI-55 as an in vivo ligand for the DA transporter. Following intravenous injection in mice, [125I]RTI-55 showed highest accumulation in areas with high densities of dopamine uptake sites. Light microscopic autoradiography was used to examine binding with higher resolution. Displacement studies demonstrated that [125I]RTI-55 binding in dopamine containing regions, striatum and olfactory tubercles, was saturable and inhibited by other cocaine analogs. GBR 12909 and WIN 35,428 significantly inhibited [125I]RTI-55 binding in striatum, while paroxetine significantly inhibited hypothalamic binding but had little effect in striatum. The latter finding suggests that [125I]RTI-55 also binds to the serotonin transporter. Haloperidol had no effect on [125I]RTI-55 binding in any brain region measured. In addition, treatment of animals with the dopamine neurotoxin MPTP caused significant reductions in striatal [125I]RTI-55 binding. The results of these studies indicate that [125I]RTI-55 binds primarily to the dopamine transporter in the mouse striatum in vivo.
Phosphine-Based <i>Z</i>-Selective Ruthenium Olefin Metathesis Catalysts (2016)

Whereas a number of highly Z-selective ruthenium-based olefin metathesis catalysts bearing N-heterocyclic carbene ligands have been reported in recent years, Zselectivity has so far been difficult to achieve for phosphinebased catalysts. Guided by predictive density functional theory (DFT) calculations, we have developed phosphine-based ruthenium olefin metathesis catalysts giving 70−95% of the Zisomer product in homocoupling of terminal alkenes such as allylbenzene, 1-octene, allyl acetate, and 2-allyloxyethanol. Starting from a moderately selective catalyst, [P(Cy)3](-S-2,4,6-Ph-C6H2)ClRu(==CH-o-OiPrC6H4) (4, Cy = cyclohexyl, iPr = isopropyl), obtained by substituting a chloride of the Hoveyda−Grubbs first-generation catalyst with 2,4,6- triphenylbenzenethiolate, we moved on to replace Cl and PCy3 by chelating, anionic phosphine ligands. Such ligands increase selectivity by limiting rotation around the P−Ru bond and by specifically directing the steric bulk of the phosphine substituents toward the selectivity-inducing thiolate ligand. In particular, DFT calculations predicted that o-(dialkylphosphino)phenolate ligands should improve selectivity and activity compared to 4. The most promising of these compounds (8b), based on the o-(ditert- butylphosphino)phenolate ligand, directs the two P-bonded tert-butyl substituents toward the 2,4,6-triphenylbenzenethiolate and has little steric hindrance trans to the thiolate. This compound metathesizes terminal olefins such as allylbenzene and 1- octene with Z-selectivities above 80% and allylacetate above 90%. Although these phosphine-based ruthenium monothiolate catalysts in general achieve somewhat lower activities and Z-selectivities than their second-generation counterparts, they also offer examples giving less substrate and product isomerization and thus higher yields.
Electro-Optical Ion Detectors in Mass Spectrometry Simultaneous Monitoring of All Ions over Wide Mass Ranges (1979)

Efficient signal collection has been a major problem in the development of observational instrumentation systems since their beginnings. One of the earliest approaches to this problem involves the utilization of photographic techniques. Light sensitivie emulsions (photographic plates) have been used for recording images at the focal point of a telescope since the middle of the 18th century. Similarly, they have been used for recording the spectra produced by various spectrographs for nearly 75 years. The ion-sensitive photo-plate has been the traditional method for recording mass spectra since Thomson (1) and, particularly, Aston (2) built their first mass spectrographs. Unfortunately, it is not free of a number of problems, as will be shown below. The efforts made to solve some of the shortcomings attending its general use have been discussed by Ahearn (3) and Honig (4). In principle, the photographic plate is ideally suited for simultaneously detecting and integrating the
<title>Restoration of images degraded by mechanical vibrations</title> (1994)

A method of calculating numerically the optical transfer function appropriate to any type of image motion and vibration, including random ones, has been developed. This method has been verified experimentally, and the close agreement justifies implementation in image restoration for blurring deriving from any type of image motion. The goal of this research is to recover the original image from its degraded version. There are many methods of image restoration based on the point spread function. One of the common methods is the Wiener filter. Here, some image restorations of synthetic degradation and physically degraded images are presented, based on a constrained least squares improvement of the original Wiener filter. The key to restoration is determination of the optical transfer function unique to each particular image motion and vibration.
Altered tumor vessel maturation and proliferation in placenta growth factor‐producing tumors: Potential relationship to post‐therapy tumor angiogenesis and recurrence (2003)

Cells in human tumor xenografts express similar levels of angiogenic growth factors before treatment. After radioimmunotherapy (RAIT) surviving tumor cells upregulate angiogenic growth factors, including placenta growth factor (PlGF), in a tumor-specific pattern. To determine the role of post-treatment PlGF expression on blood vessel recovery, tumor xenografts were assayed for post-RAIT vessel density (CD34+), proliferation (PCNA+) and maturity (SMA+ pericytes/mural cells). To further analyze the role of PlGF in blood vessel formation, PlGF-containing Matrigel implants were also assessed in a similar manner. The xenografts producing post-treatment PlGF increased CD34+ microvessel density 2- to 4-fold over untreated controls (p < 0.05) within 3 weeks of RAIT treatment. The proportion of mature microvessels (SMA+) decreased. Pericyte coverage and density of microvessels remained stable in the tumor that expressed neither PlGF nor VEGF after treatment. Hemoglobin content of PlGF-containing Matrigel implants was 5.7-fold that of anti-PlGF/anti-VEGF treated controls (Day 6, p < 0.03). The vessel density in PlGF-implants averaged 36.8 +/- 10.6/mm compared to 4.9 +/- 6.5/mm(2) in controls (p < 0.001). Vessels of PlGF-implants were lined by vWF+ cells, which were mostly flt-1+. These findings point to a role for PlGF in rapid restoration of tumor blood supply after treatment and thus, to enhanced likelihood of tumor regrowth. Likewise, the cells of primary human tumors that upregulate PlGF after treatment may be more likely to survive and form recurring tumors. Prevention of this angiogenic response to treatment may require administration of anti-angiogenic therapy during, rather than after, treatment.
Factors Limiting the Formation of Uniform and Thick Aluminum–Back-Surface Field and Its Potential (2005)

Theoretical calculations reveal that the quality of an aluminum–back-surface field (BSF) in a silicon solar cell can be improved by either increasing the thickness of the deposited aluminum (Al), peak alloying temperature, or both. However, this study shows that there is a critical temperature for a given screen-printed Al thickness, above which the BSF quality begins to degrade because of nonuniformity triggered by the agglomeration of Al-Si melt in combination with the bandgap narrowing resulting from the high doping effect in the agglomerated regions. It is found that this critical temperature decreases with the increase in the thickness of the deposited Al layer and, therefore, limits the quality and thickness of the Al-BSF that can be achieved before degradation sets in. This nonuniformity of Al-BSF is observed in the form of scattered Al bumps with thick and thin BSF regions. A combination of experimental results and model calculations is used to provide improved understanding and guidelines for choosing the optimal combination of Al thickness and alloying temperature.
Novel Positive Allosteric Modulators Bias Acetylcholine Signaling at Human M <sub>4</sub> Muscarinic Receptors (2013)

M 4 muscarinic acetylcholine receptors (mAChRs) are heavily expressed in the CNS, and activation of these receptors is thought to mediate the antipsychotic effects of the M 1 /M 4 ‐preferring agonist xanomeline. Clinical trials have shown xanomeline to be highly effective in treating the positive symptoms, negative symptoms, and cognitive deficits of schizophrenia as well as Alzheimer's type dementia. As a consequence, much interest has been placed on developing M 4 ‐selective drugs for the treatment of various forms of psychosis. To achieve robust selectivity, our group has identified M 4 ‐selective positive allosteric modulators (PAMs); these compounds have shown robust efficacy in animal models used to predict antipsychotic efficacy. In this study, we examined the ability of M 4 ‐selective PAMs to differentially modulate several intracellular signaling pathways (ERK phosphorylation, GIRK channel activation, arrestin recruitment) and differentially desensitize G‐protein‐mediated responses. Interestingly, multiple PAMs have the ability to bias the signaling of acetylcholine towards specific responses and have profound and differential effects on M 4 receptor β‐arrestin recruitment. These data indicate that M 4 allosteric ligands engender receptor conformational changes and signaling outcomes not previously described for GPCR orthosteric ligand interactions. Identification of signal bias and differential desensitization of M 4 receptors may be important for therapeutic actions of these compounds and will guide future M 4 receptor drug development efforts. Future efforts will concentrate on signaling properties that correlate with robust antipsychotic efficacy in vivo.
Molecular origins of scintillation in organic scintillators(Conference Presentation) (2016)

Organic-based scintillators are indispensable materials for radiation detection owing to their high sensitivity to fast neutrons, low cost, and tailorable properties. There has been a recent resurgence of interest in organic scintillators due to exciting discoveries related to neutron discrimination and gamma-ray spectroscopy, which represent capabilities previously thought not possible in these materials. I will discuss our development of crystalline and polymer-based scintillators for these applications. Structure-property relationships related to intermolecular interactions and host-guest electronic exchange will be discussed in the context of energy-transfer pathways relevant to scintillation. An emphasis will be placed on the rational design of these materials, as guided by first principles and DFT calculations. Two related topics will be discussed: 1) Incorporation of organometallic triplet-harvesting additives to plastic scintillator matrices to confer a 'two-state' (singlet and triplet) luminescence signature to different types of ionizing radiation. This approach relies upon energetic and spatial overlap between the donor and acceptor excited states for efficient electronic exchange. Key considerations also include synthetic modification of the luminescence spectra and kinetics, as well as the addition of secondary additives to increase the recombination efficiency. 2) Design of organotin-containing plastic scintillators as a route towards gamma-ray spectroscopy. Organometallic compounds were selected on the basis of distance-dependent quenching relationships, phase compatibility with the polymer matrix, and the gamma-ray cross sections. This approach is guided by molecular modeling and radiation transport modeling to achieve the highest possible detection sensitivity luminescence intensity.
Sorting the Garbage: Filtering Out DRDoS Amplification Traffic in ISP Networks (2019)

Distributed Reflected Denial of Service (DRDoS) attacks have been continuing to grow unprecedentedly in the recent years. Attackers abuse genuine services running some application protocols built over UDP to generate amplified traffic targeting victim network. An Internet Service Provider (ISP) may host hundreds or even thousands of hosts running these vulnerable protocols that could become amplifier nodes in DRDoS attacks. If abused, they can collectively cause large volumes of garbage amplification traffic flowing out of the ISP network. This wasteful bandwidth consumption costs the provider money and loss of Quality of Service (QoS) to its customers. Moreover, the owners of services vulnerable to amplification have to spend their resources to process illicit requests. In this paper, we propose a novel idea to filter out garbage traffic from an ISP network. We employ a special type of a honeypot that collects information about ongoing DRDoS attacks, and Software Defined Network (SDN) paradigm offering us a unified interface to deploy firewall rules on a large variety of network devices. The rules block incoming amplification requests from reaching amplifiers located within the provider network rescuing vulnerable services from being abused. This prevents garbage traffic from leaving the network enabling the provider to save money and improve QoS. Moreover, our solution also contributes to victim's liveliness because it reduces the attack traffic reaching the target network. In addition, it stimulates ISPs to implement ingress filtering best practices for all its network routers in order to minimize damage from an attacker located in the same network.
Nanocarbon Materials: Preparation and Characterization of Newly Discovered Fibrous Aggregates of Single‐Walled Carbon Nanohorns (Adv. Mater. 33/2016) (2016)

As described on page 7174, R. Yuge and co-workers succeeded in preparing novel nanocarbons. These fibrous aggregates composed of radially-assembled graphene-based single-walled nanotubules, described as fibrous aggregates of single-walled carbon nanohorns, have high dispersibility in solution, large specific surface areas, and high electrical conductivity, being suitable for high performance devices such as batteries, capacitors, fuel cells, and actuators.
Both TRIM5α and TRIMCyp have only weak antiviral activity in canine D17 cells (2007)

We show that D17 cells provide a poor environment for the inhibition of retroviral replication by proteins of the TRIM5 family. Because both TRIM5alpha and TRIMCyp are poorly active in these cells, despite having quite different viral target recognition domains, we conclude that a step either upstream or downstream of target recognition is impaired. We speculate that an unknown factor required for TRIM5alpha and TRIMCyp activity is missing or inadequately expressed in D17 cells.
Zero Lag Synchronization of Mutually Coupled Lasers in the Presence of Delays (2007)

We consider a line of three mutually coupled lasers with time delays and study chaotic synchronization of the outer lasers. Two different systems are presented: optoelectronically coupled semiconductor lasers and optically coupled fiber lasers. While the dynamics of the two systems are very different, robust synchronization of end lasers is obtained in both cases over a range of parameters. Here, we present analysis and numerical simulation to explain some of the observed synchronization phenomena. First, we introduce the system of three coupled semiconductor lasers and discuss the onset of oscillations that occurs via a bifurcation as the coupling strength increases. Next, we analyze the synchronization of the end lasers by examining the dynamics transverse to synchronized state. We prove that chaotic synchronization of the outer semiconductor lasers will occur for sufficiently long delays, and we make a comparison to generalized synchronization in driven dissipative systems. It is shown that the stability of synchronous state (as indicated by negative Lyupunov exponents transverse to the synchronization manifold) depends on the internal dissipation of the outer lasers. We next present numerical simulations for three coupled fiber lasers, highlighting some of the differences between the semiconductor and fiber laser systems. Due to the large number of coupled modes in fiber lasers, this is a good system for investigating spatio-temporal chaos. Stochastic noise is included in the fiber laser model, and synchrony of the outer lasers is observed even at very small coupling strengths.
Model Based Diagnostics and Prognosis System for Rotating Machinery (1995)

A PC-based automated mechanical vibration diagnostic and prognosis system for rotating machinery is under development by integrating AI-expert system-based interpretative capabilities with rotor dynamics based modeling and numerical optimization techniques. Presented here are the details involved while generating a rotor dynamic simulator: A turbine-generator is properly modeled using the finite element approach to compute steady-state response. The bearing stiffness and damping properties are computed by numerically solving the Reynold’s equation. An optimizer software has been interfaced with the rotor dynamics code for the solution of nonlinear unconstrained function minimization. A finite element based closed form approach has been adopted to compute the gradients of the objective function. The model is perturbed by the optimizer to match the results with simulated field measurement. The model based optimization technique has been demonstrated on a 120 mass, 6 bearing rotor system. After optimization, the responses and mass unbalance converge to their goal (field) values. To date, feasibility studies show encouraging results to differentiate between mass unbalance and misalignment for realistic systems using this methodology.
Self-contained, accurate precomputation prefetching (2015)

This work revisits precomputation prefetching targeting long access latency loads with access patterns that are hard to predict. It presents Ekivolos, a precomputation prefetcher system that automatically builds prefetching slices that contain enough control flow instructions to faithfully and autonomously recreate the program's access behavior without inducing monitoring and execution overhead on the main thread. Ekivolos departs from the traditional notion of creating optimized short slices. In contrast, it shows that even longer slices can run ahead of the main thread and perform useful prefetches as long as they are sufficiently accurate. Ekivolos operates on arbitrary application binaries and takes advantage of the observed execution paths in creating its slices. On a set of emerging workloads Ekivolos outperforms three state-of-the-art hardware prefetchers and previously proposed precomputation-based prefetchers.
Microwave soil moisture sensor based on phase shift detection of transmission coefficient in band-stop structures (2011)

In this paper novel miniature microwave soil moisture sensors based on band-stop structures have been developed, which operate at a fixed single microwave frequency. Sensors were designed in microstrip technology for use in wireless sensor networks for measurement and mapping of soil moisture in arable lands. Sensors detect transmission coefficient phase delay which is a function of the soil permittivity that is in turn in direct relation with soil moisture. Two novel sensors are proposed which operate at 2.54 GHz and 2.75 GHz. Both solutions offer two times wider ranges of the phase delay and from three to almost thirteen times greater sensitivities compared to conventional microstrip sensor solutions.
Disease modifying and antiangiogenic activity of 2-Methoxyestradiol in a murine model of rheumatoid arthritis (2009)

These data demonstrate that in the CAIA mouse model of RA, 2ME2 has disease modifying activity that is at least partially attributable to the inhibition of neovascular development. Further, the data suggests new mechanistic points of intervention for 2ME2 in RA, specifically inhibition of inflammatory mediators and osteoclast activity.
Is There Any Association Between Clinical Features or IBD Seromarker Expression and the Efficacy of Aggressive Medical Therapy of de novo Crohnʼs Disease after Ileal Pouch-Anal Anastomosis? (2009)

Purpose: About 5%-10% of patients with ulcerative colitis (UC) who undergo ileal pouch-anal anastomosis (IPAA) subsequently develop de novo Crohn's disease (CD). Most physicians use a “step-up” approach to medical treatment of de novo CD after IPAA starting with antibiotics, then escalating to 5-ASA products, corticosteroids, immunodulators and biologics. There is little published literature on how effectively medical therapies can salvage CD pouches and avoid permanent ileostomy. In this study, we assessed the effectiveness of medical therapy of de novo CD after IPAA, and investigated whether any clinical or serologic factors were associated with the need for permanent ileostomy and pouch failure (PF). Methods: A prospectively generated clinical database of UC and IC patients who underwent IPAA by a single surgeon was queried for patients who subsequently developed de novo CD. Clinical features and seromarker expression (pANCA, ASCA-IgG, ASCA-IgA, anti-OmpC, anti-CBirl, anti-I2) was assessed before surgery. Clinical phenotypes of de novo CD included inflammatory (pouch or afferent ileal limb inflammation), fistulizing (pouch fistulizing disease), or anal disease. Medications used as pouch salvage (PS) interventions were recorded. PF was defined as the need for permanent ileostomy after failure to respond to medical therapy. Results: Forty patients (21 males and 19 females) with a median age of 33 yr (range, 12-71 yr) comprised the study group. There were 31 patients (78%) with inflammatory CD, 5 patients (13%) with pouch fistulizing CD, and 4 patients (10%) with anal disease. Median follow-up time of the study cohort was 34 months (range, 4 to 132 months). Medical PS was successful in 34 patients (85%) with antibiotics alone (n=22), immunomodulators (n=7) and biologics (n=5). Six patients (15%) failed anti-TNF therapy and and developed PF. Median time to permanent ileostomy was 17 months (range, 0 to 103 months). The incidence of PF was 13% in de novo inflammatory CD, 0% in de novo fistulizing CD and 50% in de novo anal CD (p=0.1). No pre- or post-operative clinical variable was associated with PF. Preoperatively most patients expressed the UC-associated pANCA (78%); CD-associated seromarkers of ASCA-IgG, ASCA-IgA, anti-OmpC, anti-CBirl and anti-I2 were detected in 3%, 13%, 25%, 18% and 18%, respectively. No statistically significant associations were noted between any individual or combination of seromarkers and PF. Conclusion: Aggressive medical therapy of de novo CD after IPAA can avoid permanent ileostomy in 85% of cases. Early results from this prospective study suggest that no clinical or serologic variables appear to be associated with pouch failure in medically treated patients with de novo CD after IPAA. Disclosure: Dr Targan - Founder Prometheus Lab Dr Vasiliauskas - Speakers Bureau, Prometheus Labs.
High-Power/High-Temperature CW Narrow-Ridge Mid-Infrared Interband Cascade Lasers (2007)

Mid-infrared interband cascade lasers with a 12-mμ-wide ridge and Au electroplating for improved epitaxial-side-up heat sinking operated cw up to 257 K and produced 100 mW/facet at 80 K. A distributed-feedback laser emitted 40 mW of cw power into a single mode.