gebhart/patrepeval huggingface dataset:
Dopamine D<sub>3</sub> and D<sub>4</sub> Receptor Antagonists:  Synthesis and Structure−Activity Relationships of (<i>S</i>)-(+)-<i>N</i>-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl)amino]-2-methoxybenzamide (YM-43611) and Related Compounds (1996)

In this study, we synthesized a series of (S)-N-(3-pyrrolidinyl)benzamide derivatives, 1, 2a−d, 5a−l, and 7, and their enantiomers, (R)-1 and (R)-5c−e, and evaluated their binding affinity for cloned dopamine D2, D3, and D4 receptors and their inhibitory activity against apomorphine-induced climbing behavior in mice. The results indicate that D2, D3, and D4 receptors have different bulk tolerance (D4 > D3 > D2) for the substituent of the 4-amino group (R1) on the benzamide nuclei and that cyclopropyl-, cyclobutyl-, and cyclopentylcarbonyl groups likely possess adequate bulkiness with respect to D3 and D4 affinity and selectivity over D2 receptors in this series. The results also suggested that the N-substituent (R2) on the pyrrolidin-3-yl group performs an important role in expressing affinity for D2, D3, and D4 receptors and selectivity among the respective subtypes. One of the compounds, (S)-(+)-N-(1-benzyl-3-pyrrolidinyl)-5-chloro-4-[(cyclopropylcarbonyl)amino]-2-methoxybenzamide (5c) (YM-43611), showed high affinity for D3 and D4 receptors (Ki values of 21 and 2.1 nM, respectively) with 110-fold D4 selectivity and 10-fold D3 preference over D2 receptors and weak or negligible affinity for representative neurotransmitter receptors. Compound 5c displayed potent antipsychotic activity in inhibiting apomorphine-induced climbing behavior in mice (ED50 value, 0.32 mg/kg sc).
In vivo 31P nuclear magnetic resonance spectroscopy of bone mineral for evaluation of osteoporosis. (1988)

The mineral content of stationary bone samples can be quantified by 31P nuclear magnetic resonance (NMR) spectroscopy. The assay can be performed in regions of the anatomy that pose problems for absorptiometric techniques, because the mineral content is measured within a selected volume without concern for the geometry of the bone. In vivo 31P NMR spectra of the bones in human fingers and wrist are reported. Soft tissue such as marrow and skeletal muscle contributes little to the 31P NMR spectra of human fingers and wrist and thus should not seriously affect the accuracy of the mineral assay. 31P NMR spectrometry should prove helpful for confirming rapid bone mineral loss in those at risk and for monitoring response to treatment.
Chemical modification of fortimicins III. Preparation of N-substituted fortimicin A derivatives. (1981)

The 1, 2' or 6'-amino group of fortimicin A was alkylated or acylated and the antimicrobial activities of the derivatives were compared with each other. 2'-N-Substituted fortimicins A were active against the fortimicin A resistant strain which produced AAC(3)-I. AAC(3)-I is the only enzyme which can inactivate fortimicin A. Among the derivatives prepared in the present study, 2'-N-[(S)-4-amino-2-hydroxybutyl]fortimicin A showed stronger activity than fortimicin A.
Functional Consequences of Posttranslational Isomerization of Ser <sup>46</sup> in a Calcium Channel Toxin (1994)

The venom of the funnel-web spider Agelenopsis aperta contains several peptides that paralyze prey by blocking voltage-sensitive calcium channels. Two peptides, omega-Aga-IVB (IVB) and omega-Aga-IVC (IVC), have identical amino acid sequences, yet have opposite absolute configurations at serine 46. These toxins had similar selectivities for blocking voltage-sensitive calcium channel subtypes but different potencies for blocking P-type voltage-sensitive calcium channels in rat cerebellar Purkinje cells as well as calcium-45 influx into rat brain synaptosomes. An enzyme purified from venom converts IVC to IVB by isomerizing serine 46, which is present in the carboxyl-terminal tail, from the L to the D configuration. Unlike the carboxyl terminus of IVC, that of IVB was resistant to the major venom protease. These results show enzymatic activities in A. aperta venom being used in an unprecedented strategy for coproduction of necessary neurotoxins that possess enhanced stability and potency.
Quarter-Rate Superconducting Modulator for Improved High Resolution Analog-to-Digital Converter (2007)

We describe the design of a new oversampled analog-to-digital converter (ADC) based on phase modulation-demodulation (PMD) architecture. In a PMD ADC, the analog input signal modulates the phase of a periodic stream of fluxons applied to a modulator circuit for subsequent demodulation in a clocked synchronizer circuit to produce a digital code. The new modulator provides a way to quadruple the average fluxon transport rate, and hence the input dynamic range, by replacing the single junction interferometer with a high-speed symmetric divide-by-4 circuit. The divider acts as a 1:4 asynchronous demultiplexer which distributes incoming fluxons among its four quarter-rate outputs. This four-fold rate reduction, at the modulator output, allows one to increase the ADC maximum input slew rate to 2 fluxons per clock period, achieving 2 additional bits of resolution at the same sampling clock frequency. We have designed and fabricated a quarter-rate ADC front-end and present low frequency test results for the same. The ADC comprises a quarter-rate quantizer which has been successfully tested at an input frequency of 81.92 GHz.
Spatiotemporal Interactions in Retinal Prosthesis Subjects (2010)

During multielectrode stimulation, interactions between electrodes have a significant influence on the quality of the percept. Understanding how these spatiotemporal interactions at the neural level influence percepts during multielectrode stimulation is fundamental to the successful design of a retinal prosthesis.
Human Rotavirus Type 2: Cultivation in Vitro (1980)

A strain of type 2 human rotavirus (Wa) was grown to relatively high titer through 14 passages in primary cultures of African green monkey kidney (AGMK) cells. This passage series was initiated with virus that had been passaged 11 times serially in newborn gnotobiotic piglets. In contrast, virus present in the stool of patient Wa as well as virus from the first, second, or third passage in piglets could not be propagated successfully in African green monkey kidney cells. Prior to each passage in cell culture, the virus was treated with trypsin and the inoculated cultures were centrifuged at low speed. Cultivation of a type 2 human rotavirus should aid attempts to characterize this virus and to develop a means of immunoprophylaxis for a serious diarrheal disease of human infants.
Genetic Analysis of Fusion Recombinants and Presence of Noncomplementing Diploids in Bacillus megaterium (1985)

We have attempted to undertake genetic analysis in Bacillus megaterium using the technique of protoplast fusion that has been successfully applied in Staphylococcus and Streptomyces. Efficient production of protoplasts, fusion and regeneration techniques have been established. However, variability in numbers and types of recombinants using two-, three-, and four-factor crosses was observed throughout these studies. No linkages were detected, even between loci known to be linked by cotransduction with bacteriophage MP13. These results were similar to those reported by Alföldi and coworkers using B. megaterium strain 216, even though the experimental design was significantly changed. During initial subculturing, segregants were observed in a 1:2:2 ratio of noncomplementing diploids:parental-1:parental-2. The ratio changed dramatically after seven subcultures. Double recombinants appeared after nine subcultures. These results corroborate those reported in B. subtilis and suggest that there is a locus-inactivation phenomenon present in Bacillus which is not evident in Streptomyces or Staphylococcus. Until the mechanism is elucidated, protoplast fusion should not be used for chromosomal mapping in B. megaterium. However, it can be used to transfer plasmids among the bacilli at a frequency of 10(-5)-10(-6) per regenerated protoplast.
Integration of Pneumatic Technology in Powered Mobility Devices (2017)

Advances in electric motors, electronics, and control systems have enhanced the capability and drivability of electric power mobility devices over the last 60 years. Yet, battery technologies used in powered mobility devices (PMDs) have not kept pace. Recent advances in pneumatic technology, primarily the high torque, low speed design of rotary piston air motors, directly align with the needs of PMD. Pneumatic technology has advantages over battery-powered technology, including lighter weight, lower operating costs, decreased environmental impact, better reliability, and increased safety. Two prototypes were created that incorporated rotary piston air motors, high-pressure air tanks, and air-pressure regulators. Prototype 1 was created by modifying an existing electric PMD. Range tests were performed to determine the feasibility of pneumatic technology and the optimal combination of components to allow the longest range possible at acceptable speeds over ideal conditions. Using a 1.44 L air tank for feasibility testing, prototype 1 was capable of traveling 800 m, which confirmed the feasibility of pneumatic technology usage in PMDs. Prototype 2 was designed based on the testing results from prototype 1. After further optimization of prototype 2, the average maximum range was 3,150 m. Prototype 2 is up to 28.3% lighter than an equivalent size electric PMD and can be fully recharged in approximately 2 minutes. It decreases the cost of PMDs by approximately $1,500, because batteries do not need to be replaced over the lifetime of the device. The results provide justification for the use of pneumatic technology in PMDs.
Performance Analysis of the Postcomputation- Based Generic-Point Parallel Scalar Multiplication Method (2010)

A Postcomputation-based generic-point parallel scalar multiplication method has recently been proposed for high-performance end servers 

that employ parallel elliptic curve cryptoprocessors. The sequential precomputation overheads, in the postcomputation-based method, are replaced with 

parallelizable postcomputations. This paper analyzes the performance of the postcomputation-based method with 128 ≤ m ≤ 256 using a number of parallel elliptic curve cryptoprocessors. The results show that the best performance is achieved when eight cryptoprocessors are used.
User Multiplexing in Relay Enhanced LTE-Advanced Networks (2010)

The 3 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">rd</sup> Generation Partnership Project has recently started the standardization process for LTE-Advanced, as a major evolution step of UTRAN LTE Release 8. One of the key enhancing technologies being studied that may help to fulfill the challenging performance targets of LTE-Advanced networks is radio relaying. This uses relay nodes that act as surrogate base stations for mobile users whose radio links with the base stations are not experiencing good enough conditions. In the downlink, the data that is destined for the relayed users may first have to be multiplexed by the base station, sent over the wireless backhaul link towards the relay node, and de-multiplexed and forwarded to the individual users by the relay node. The reverse process also has to be undertaken in the uplink. In this paper, we present a novel multiplexing scheme which is able to adapt the addressing and bitmapping of user identification to the actual number of users being served by the relay nodes, and thus greatly reduce the multiplexing overhead.
Monoclonal antibodies: a morphing landscape for therapeutics (2006)

Abstract The concept of using antibodies as therapeutics to cure human diseases was postulated nearly 100 years ago by Paul Ehrlich and subsequently enabled by the discovery of hybridoma technology by Kohler and Milstein in 1975. While the use of monoclonal antibodies (mAbs) as drugs that can specifically target a disease‐associated antigen is compelling, it has taken a quarter century for these molecules to be adopted as bona fide therapeutic agents. Despite their slow pursuit in drug development during the pioneering years, it is now estimated that there are nearly 500 mAb‐based therapies in development. Major factors that have influenced the acceptance of monoclonal antibodies as therapeutics include their drug safety profiles, technological advancements for facilitating mAb discovery and development, and market success. Early on, it was demonstrated that antibodies could elicit clinical benefit by antagonizing a specific antigen without the common side effects that are prevalent with small chemical entities due to their nonspecific effects on homeostatic biochemical pathways. In addition, the significant technological advances that the biotechnology industry has established for developing and producing monoclonal antibodies at commercial scale in a more efficient and cost‐effective manner has broadly enabled their use as therapeutics. However, despite the beneficial pharmacologic advantages and technological advances, it has been the sheer market success that monoclonal antibody products have achieved over the past few years that has propelled their vast pursuit by the biopharmaceutical industry in light of their value‐creating potential. Here we provide an overview of the monoclonal antibody industry and discuss evolving technologies and strategies that are being pursued to overcome challenges in the changing marketplace. Drug Dev. Res. 67:781–789, 2006. © 2007 Wiley‐Liss, Inc.
<title>Threshold characteristics of an OASLM using a a-Si:H photoconductor and a SSFLC modulator</title> (1993)

We present the write light intensity threshold characteristics of an OASLM incorporating a hydrogenated amorphous silicon photoconductor and a surface stabilized ferroelectric liquid crystal modulator, LAPS-SLM. In this paper, we describe a new implementation which applying the two threshold characteristics of the LAPS-SLM to perform all Boolean logic by one device.© (1993) COPYRIGHT SPIE--The International Society for Optical Engineering. Downloading of the abstract is permitted for personal use only.
Current evaluation of the tissue localization and diagnostic utility of prostate specific membrane antigen (1998)

BACKGROUND Current statistics indicate that prostate carcinoma is the most common form of cancer diagnosed in American men, resulting in the second highest cancer death rate. Early diagnosis and accurate staging are imperative given that there is little effective treatment for metastatic disease, especially after androgen deprivation therapy fails. Identification of new biochemical markers for disease progression will provide important tools for diagnosis and monitoring. One such potential marker is prostate specific membrane antigen (PSMA). METHODS A review was conducted to identify reports concerning evaluation of diagnostic applications of PSMA. RESULTS PSMA is a membrane-bound glycoprotein that is highly restricted to the prostate. Immunohistochemical findings indicate that PSMA is a marker of epithelial cells of the prostate. This expression is increased in association with prostate carcinoma, particularly in hormone-refractory disease. Given its membrane-bound character, PSMA has been exploited as a marker for tumor detection by immunoscintiscanning with the 111In-labeled anti-PSMA monoclonal antibody 7E11.C5. Increased concentrations of 7E11.C5-reactive antigen are present in the serum of prostate carcinoma patients compared with healthy individuals; also, hematogenous circulating prostate carcinoma cells are detectable with reverse transcriptase-polymerase chain reaction analysis with primers specific for PSMA. New monoclonal antibodies specific for extracellular portions of the PSMA molecule currently are being utilized in applied studies. CONCLUSIONS PSMA is a widely used marker for prostate epithelial cells. Its up-regulation in association with cancer, particularly in advanced cancer, is ideal for application as a prognostic marker. A variety of promising clinical applications utilizing PSMA have been or are being developed. In the future, these promise to have an important impact on cancer diagnosis and patient treatment. Cancer 1998;83:2259-2269. © 1998 American Cancer Society.
Pulse separation control for mode-locked far-infrared <i>p</i>-Ge lasers (1999)

Active mode locking of the far-infrared p-Ge laser giving a train of 200 ps pulses is achieved via gain modulation by applying an rf electric field together with an additional bias at one end of the crystal parallel to the Voigt-configured magnetic field. Harmonic mode locking yields a train of pulse pairs with variable time separation from zero to half the roundtrip period, where pulse separation is electrically controlled by the external bias to the rf field.
A recombinant single-chain IL-7/HGFβ hybrid cytokine induces juxtacrine interactions of the IL-7 and HGF (c-Met) receptors and stimulates the proliferation of CFU-S12, CLPs, and pre-pro-B cells (2005)

A novel recombinant interleukin-7/hepatocyte growth factor beta-chain (IL-7/HGFbeta) hybrid cytokine was constructed as a single chain (sc) composed of IL-7 and HGFbeta connected by a flexible linker. Unlike recombinant (r) IL-7, which stimulated pro-B cells and pre-B cells only, scIL-7/HGFbeta stimulated the proliferation of pre-pro-B cells, common lymphoid progenitors (CLPs), and colony-forming unit (CFU)-S12 in cultures of IL-7-/- mouse BM cells. When injected in vivo, 3- to 4-fold more splenic B-lineage cells appeared in recipients of bone marrow (BM) cells from the scIL-7/HGFbeta-stimulated cultures than from rIL-7-stimulated cultures. Moreover, on a per-cell basis, scIL-7/HGFbeta culture-generated cells produced 16- to 20-fold more BM and splenic B-lineage cells than did normal BM cells. Antibody blocking, receptor phosphorylation, and confocal microscopy demonstrated that scIL-7/HGFbeta signals though both the IL-7 and HGF (c-Met) receptors, which form IL-7R/c-Met complexes on the surface of CLPs and pre-pro-B cells. In addition, the IL-7Ralpha chain, gammac chain, and c-Met were coisolated from purified CLPs and pre-pro-B cells on scIL-7/HGFbeta affinity gels, indicating that they are major components of the IL-7/HGFbeta receptor. Hence, the present results demonstrate that the IL-7/HGFbeta hybrid cytokine efficiently and selectively stimulates the most primitive B-lineage precursors in BM by inducing juxtacrine interactions between the IL-7 and c-Met receptors.
Adiabatic elimination-based coupling control in densely packed subwavelength waveguides (2015)

The ability to control light propagation in photonic integrated circuits is at the foundation of modern light-based communication. However, the inherent crosstalk in densely packed waveguides and the lack of robust control of the coupling are a major roadblock toward ultra-high density photonic integrated circuits. As a result, the diffraction limit is often considered as the lower bound for ultra-dense silicon photonics circuits. Here we experimentally demonstrate an active control of the coupling between two closely packed waveguides via the interaction with a decoupled waveguide. This control scheme is analogous to the adiabatic elimination, a well-known procedure in atomic physics. This approach offers an attractive solution for ultra-dense integrated nanophotonics for light-based communications and integrated quantum computing.
Coverage Verification without Location Information (2011)

Wireless sensor networks (WSNs) have recently emerged as a prominent technology for environmental monitoring and hazardous event detection. Yet, their success depends considerably on their ability to ensure reliable event detection. Such guarantees can be provided only if the target field monitored by a WSN does not contain coverage holes that are not monitored by any sensor. Currently, the coverage hole detection solutions require accurate knowledge of the sensors locations, which cannot be easily obtained, or they cannot provide guarantees on the coverage quality. In this study, we address the challenge of designing an accurate k-coverage verification scheme, without using location information, for a predefined k\ge 1. To this end, we present two efficient, distributed, and localized k-coverage verification schemes with proven guarantees on their coverage detection quality. Our simulations show that the schemes accurately detect coverage holes of various sizes.
Preparation of semiconductor devices by ionized-cluster beam deposition and epitaxy (1976)

It is shown that the ionized-cluster beam deposition and epitaxial techniques are useful for the semiconductor device fabrications. In this technique, the vapour, on emerging from the nozzle, is partially condensed into clusters with the Van der Waals force. The clusters are then ionized by electron bombardment and accelerated onto the substrate. The deposited film shows good adhesion, good conductive even in a very thin film, and good crystalline state. These techniques are applied to ohmic contact, interconnection, and semiconductor material preparation for devices and ICs.
Electrical energy storage using compressed gas in depleted hydraulically fractured wells (2021)

Renewable forms of electricity generation like solar and wind require low-cost energy storage solutions to meet climate change deployment goals. Here, we explore the use of depleted hydraulically fractured ("fracked") oil and gas wells to store electrical energy in the form of compressed natural gas to be released to spin an expander/generator when electrical demand is high. Our reservoir model indicates that the same dual-porosity geological environment of fracked wells used to liberate hydrocarbons is also suitable for storing and releasing gas in a diurnal or seasonal cycle. Round-trip storage efficiency is calculated to be 40%-70% depending on the natural reservoir temperature. Levelized cost of storage is estimated to be $70-270/MWh, on par with pumped hydro storage. This study indicates that repurposed "fracked" wells could provide a much-needed low-cost seasonal energy storage solution at the TWh scale.
Method of detecting sulfur dioxide. [DOE patent application; 1,1,1-trimethyl-N-sulfinyl silanamine] (1981)

(CH/sub 3/)/sub 3/SiNSO is produced by the reaction of ((CH/sub 3/)/sub 3/Si)/sub 2/NH with SO/sub 2/. Also produced in the reaction are ((CH/sub 3/)/sub 3/Si)/sub 2/O and a new solid compound (NH/sub 4/)((CH/sub 3/)/sub 3/SiOSO/sub 2/). Both (C/sub 3/)/sub 3/SiNSO and (NH/sub 4/)((CH/sub 3/)/sub 3/SiOSO/sub 2/) have fluorescent properties. The reaction of the subject invention is used in a method of measuring the concentration of SO/sub 2/ pollutants in gases. By the method, a sample of gas is bubbled through a solution of ((CH/sub 3/)/sub 3/Si)/sub 2/NH, whereby any SO/sub 2/ present in the gas will react to produce the two fluorescent products. The measured fluorescence of these products can then be used to calculate the concentration of SO/sub 2/ in the original gas sample. The solid product (NH/sub 4/)((CH/sub 3/)/sub 3/SiOSO/sub 2/) may be used as a standard in solid state NMR spectroscopy.
Ranging likelihood for wideband wireless localization (2013)

High-accuracy localization in harsh environments is a challenging research problem, mainly due to non-line-of-sight (NLOS) propagation, multipath effect, and multiuser interference. Many techniques have been proposed to address this problem; most of them focus on improving the accuracy of ranging estimation, e.g., NLOS identification and mitigation. In this paper, we take ranging one step further by introducing the concept of ranging likelihood (RL), showing that RL is the essential element for localization. Moreover, we present effective techniques for real-time RL estimation. We focus on ultra-wide bandwidth (UWB) localization systems and assess the performance of the proposed approach by using the data from an extensive indoor measurement campaign. The results show that the proposed approach can significantly improve the performance of wireless localization in harsh environments.