gebhart/patrepeval huggingface dataset:
Design and Synthesis oftrans-3-(2-(4-((3-(3-(5-Methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro- 1H-3-benzazepine (SB-414796):  A Potent and Selective Dopamine D3Receptor Antagonist (2003)

At their clinical doses, current antipsychotic agents share the property of both dopamine D(2) and D(3) receptor blockade. However, a major disadvantage of many current medications are the observed extrapyramidal side-effects (EPS), postulated to arise from D(2) receptor antagonism. Consequently, a selective dopamine D(3) receptor antagonist could offer an attractive antipsychotic therapy, devoid of the unwanted EPS. Using SAR information gained in two previously reported series of potent and selective D(3) receptor antagonists, as exemplified by the 2,3,4,5-tetrahydro-1H-3-benzazepine 10 and the 2,3-dihydro-1H-isoindoline 11, a range of 7-sulfonyloxy- and 7-sulfonylbenzazepines has been prepared. Compounds of this type combined a high level of D(3) affinity and selectivity vs D(2) with an excellent pharmacokinetic profile in the rat. Subsequent optimization of this series to improve selectivity over a range of receptors and reduce cytochrome P450 inhibitory potential gave trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxidiazolyl))phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (58, SB-414796). This compound is a potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and is CNS penetrant in the rat. Subsequent evaluation in the rat has shown that 58 preferentially reduces firing of dopaminergic cells in the ventral tegmental area (A10) compared to the substantia nigra (A9), an observation consistent with a prediction for atypical antipsychotic efficacy. In a separate study, 58 has been shown to block expression of the conditioned place preference (CPP) response to cocaine in male rats, suggesting that it may also have a role in the treatment of cue-induced relapse in drug-free cocaine addicts.
Image processing on compressed data for large video databases (1993)

This paper presents a novel approach to processing encoded video sequences prior to decoding. Scene changes may be easily detected using DCT coefficients in JPEG and MPEG encoded video sequences. In addition, by analyzing the DCT coefficients, regions of interest may be isolated prior to decompression, increasing efficiency of any subsequent image processing steps, such as edge detection. The results are currently used in a video browser, and are part of an ongoing research project in creating large video databases. The procedure is presented in detail and several examples are exhibited.
Socio-economic development and transition in the duration of post-partum amenorrhoea: survival function analysis of data. (1990)

The impact of improved maternal socioeconomic status in the form of nutritious food on length of postpartum amenorrhea (PPA) is assessed using data for Varanasi city, India, for the period 1987-1990. "Estimates of survival functions corresponding to data relating to mothers of different social status groups, assumed to represent health condition of mothers, are obtained and compared. Finally, it is concluded that the distribution of duration of PPA is a mixture of two distributions and it differs from one social status group to [the] other."
An Expanded Definition of the Adult Respiratory Distress Syndrome (1988)

"An Expanded Definition of the Adult Respiratory Distress Syndrome." American Review of Respiratory Disease, 138(3), pp. 720–723
Outer Membrane Protein Vesicle Vaccines for Meningococcal Disease (2003)

Alternative strategies exist for prevention of group B Neisseria meningitidis (meningococcal) disease through vaccination (see Chapters 5 , 8 , 13 , 14 in this volume). However, the most promising approach to date has been the use of outer-membrane vesicle (OMV) vaccines for induction of bactericidal antibodies against cell-surface outer-membrane proteins (OMPs).
Miniature atomic magnetometer integrated with flux concentrators (2009)

High permeability magnetic flux concentrators are used to enhance the sensitivity of an atomic magnetometer operating in the spin-exchange relaxation-free regime. The magnetometer uses a millimeter scale Rb87 vapor cell and either mu-metal or Mn–Zn ferrite flux concentrators. The measured sensitivity gives excellent agreement with calculations of thermal noise from the concentrator material. The mu-metal concentrators allow a sensitivity of 50fTHz−1∕2, limited by thermal current magnetic noise. The ferrite concentrators are limited by thermal magnetization noise at low frequencies, and reach a sensitivity of 10fTHz−1∕2 for frequencies above 125Hz.
QSAR and Molecular Modelling for a Series of Isomeric X‐Sulfanilamido‐1‐phenylpyrazoles (1993)

Abstract The influence of large substituents in o‐, m‐ and p‐positions of the phenyl ring of isomeric 3‐, 4‐ and 5‐sulfanilamido‐1‐phenylpyrazoles on their inhibitory effect against E.coli derived dihydropteroic acid synthase and whole cell E.coli has been studied. According to their pKa values, the 3‐ and 5‐series show high antibacterial activity while the 4‐series displays feeble inhibitory activity. In the 3‐series the variation in MIC is explained by differences in pKa (Hammett σ) and molecular weight (MW) or substituent surface respectively, whereas in the 5‐series steric effects of substituents in the o‐position of the 1‐phenyl ring and MW describe the differences in whole cell activity. In the cell‐free system the inhibitory activity depends for the 3‐series solely on pKa or Hammett σ, respectively, and in the 5‐series, where the derivatives are almost completely ionized, the variation is solely explainable by the steric effect of the substituents in o‐position. The steric effect of o‐substituents in the 5‐series has been studied and explained by NMR‐ and molecular modelling techniques. The observed differences in electronic effects of substituents comparing the 3‐ and 4‐series with the 5‐series could be explained by the results of quantum chemical calculations.
Immune Responses in Asymptomatic HIV-1-Infected Patients After HIV-DNA Immunization Followed by Highly Active Antiretroviral Treatment (1999)

Intensive chemotherapy is capable of reducing the viral load in HIV-1-infected individuals while infected cells are still present. A special property of DNA immunization is to induce both new CTL and Ab responses. We evaluated the possibility of inducing new immune responses in already infected individuals by means of DNA constructs encoding the nef, rev, or tat regulatory HIV-1 genes. Significant changes in viral loads and CD4+ counts were observed in four patients who started highly active antiretroviral treatment (HAART) during the immunization study. The DNA immunization induced Ag-specific T cell proliferation, which persisted up to 9 mo after the last DNA injection, and cytolytic activities but did not, by itself, reduce viral load. Increased levels of CTL precursor cells were induced in all nine DNA-immunized patients. The profile of IFN-gamma secretion observed when human PBMC were transfected with the nef, rev, and tat DNA resembled that found in the CTL activity (nef > tat > rev). Ab responses that occurred after immunizations were of a low magnitude. In accordance with the high IL-6 production induced by the nef DNA plasmid, IgG titers were highest in patients immunized with nef DNA. The initiation of HAART appears to contribute to the induction of new HIV-specific CTL responses, but by itself did not cause obvious re-induction of these activities.
Synthesis and Applications of tert-Butanesulfinamide (2010)

ADVERTISEMENT RETURN TO ISSUEPREVReviewNEXTSynthesis and Applications of tert-ButanesulfinamideMaryAnn T. Robak†, Melissa A. Herbage†, and Jonathan A. Ellman*View Author Information Department of Chemistry, University of California, Berkeley, California 94720* E-mail: [email protected]†These authors contributed equally to this work.Cite this: Chem. Rev. 2010, 110, 6, 3600–3740Publication Date (Web):April 26, 2010Publication History Received18 November 2009Published online26 April 2010Published inissue 9 June 2010https://pubs.acs.org/doi/10.1021/cr900382thttps://doi.org/10.1021/cr900382treview-articleACS PublicationsCopyright © 2010 American Chemical SocietyRequest reuse permissionsArticle Views73203Altmetric-Citations978LEARN 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 SUBJECTS:Addition reactions,Amines,Molecular structure,Reagents,Stereoselectivity Get e-Alerts
Improved 8-channel silicon mode demultiplexer with grating polarizers (2014)

An improved 8-channel silicon mode demultiplexer is realized with TE-type and TM-type grating polarizers at the output ends, and these gratings serve as fiber-chip couplers simultaneously. The present 8-channel silicon mode demultiplexer includes a three-waveguide PBS (for separating the TE0 and TM0 modes) and six cascaded ADCs (for demultiplexing the high-order modes of both polarizations). The grating polarizers with high extinction ratios are used to filter out the polarization crosstalk in the 8-channel hybrid multiplexer efficiently and the measured crosstalk for all the mode-channels of the improved 8-channel mode multiplexer is reduced greatly to ~-20dB in a ~100nm bandwidth.
An Efficient Framework for Implementing Persist Data Structures on Remote NVM. (2018)

The byte-addressable Non-Volatile Memory (NVM) is a promising technology since it simultaneously provides DRAM-like performance, disk-like capacity, and persistency. In this paper, we rethink the current symmetric NVM deployment which directly attaches NVM devices with servers. Following the trend of disaggregation, we propose \emph{rNVM}, a new asymmetric deployment of NVM devices, that decouples servers from persistent data storage. In this architecture, the NVM devices can be shared by multiple servers and provide recoverable persistent data structures. We develop a prototype of \emph{rNVM} leveraging the advantages of the powerful RDMA-enabled network that naturally fits the asymmetric deployment model. With several optimizations, we demonstrate that \emph{rNVM} can achieve comparable performance as symmetric deployment while enjoying the benefits of the large data size not limited by local memory, high availability and shared data structures. Specifically, thanks to operation batching, local memory caching and efficient concurrency control, the throughput of operations on eight widely used data structures is improved by 6$\sim$22 $\times$ without lowering the consistency promising.
Photochemical Nitric Oxide Precursors:  Synthesis, Photochemistry, and Ligand Substitution Kinetics of Ruthenium Salen Nitrosyl and Ruthenium Salophen Nitrosyl Complexes1 (2002)

Described are syntheses, characterizations, and photochemical reactions of the nitrosyl complexes Ru(salen)(ONO)(NO) (I, salen = N,N'-ethylenebis(salicylideneiminato) dianion), Ru(salen)(Cl)(NO) (II), Ru((t)Bu(4)salen)(Cl)(NO) (III,(t)Bu(4)salen = N,N'-ethylenebis(3,5-di-tert-butylsalicylideneiminato) dianion), Ru((t)Bu(4)salen)(ONO)(NO) (IV), Ru((t)Bu(2)salophen)(Cl)(NO) (V, (t)Bu(2)salophen = N,N'-1,2-phenylenediaminebis(3-tert-butylsalicylideneiminato) dianion), and Ru((t)Bu(4)salophen)(Cl)(NO) (VI, (t)Bu(4)salophen = N,N'-1,2-phenylenebis(3,5-di-tert-butylsalicylideneiminato) dianion). Upon photolysis, these Ru(L)(X)(NO) compounds undergo NO dissociation to give the ruthenium(III) solvento products Ru(L)(X)(Sol). Quantum yields for 365 nm irradiation in acetonitrile solution fall in a fairly narrow range (0.055-0.13) but decreased at longer lambda(irr). The quantum yield (lambda(irr) = 365 nm) for NO release from the water soluble complex [Ru(salen)(H(2)O)(NO)]Cl (VII) was 0.005 in water. Kinetics of thermal back-reactions to re-form the nitrosyl complexes demonstrated strong solvent dependence with second-order rate constants k(NO) varying from 5 x 10(-4) M(-1) s(-1) for the re-formation of II in acetonitrile to 5 x 10(8) M(-1) s(-1) for re-formation of III in cyclohexane. Pressure and temperature effects on the back-reaction rates were also examined. These results are relevant to possible applications of photochemistry for nitric oxide delivery to biological targets, to the mechanisms by which NO reacts with metal centers to form metal-nitrosyl bonds, and to the role of photochemistry in activating similar compounds as catalysts for several organic transformations. Also described are the X-ray crystal structures of I and V.
Piezoelectric Aluminum Nitride Vibrating Contour-Mode MEMS Resonators (2006)

This paper reports theoretical analysis and experimental results on a new class of rectangular plate and ring-shaped contour-mode piezoelectric aluminum nitride radio-frequency microelectromechanical systems resonators that span a frequency range from 19 to 656 MHz showing high-quality factors in air (Q <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">max</sub> =4300 at 229.9 MHz), low motional resistance (ranging from 50 to 700 Omega), and center frequencies that are lithographically defined. These resonators achieve the lowest value of motional resistance ever reported for contour-mode resonators and combine it with high Q factors, therefore enabling the fabrication of arrays of high-performance microresonators with different frequencies on a single chip. Uncompensated temperature coefficients of frequency of approximately -25 ppm/degC were also recorded for these resonators. Initial discussions on mass loading mechanisms induced by metal electrodes and energy loss phenomenon are provided
Teratogenicity and toxicity of ethylene glycol monomethyl ether (2‐methoxyethanol) in Drosophila melanogaster: Involvement of alcohol dehydrogenase activity (1989)

Ethylene glycol monomethyl ether (EGME) or 2-methoxyethanol (2-ME) is a toxic compound that has teratogenic effects in developing organisms similar to its oxidation product methoxyacetic acid (MAA). Alcohol dehydrogenase (ADH) is supposed to be involved with the oxidation of EGME into MAA. It has been shown here that Drosophila ADH dehydrogenates EGME in an in vitro test system. Three strains of Drosophila melanogaster, genetically different from each other with regard to ADH activities (qualitatively and quantitatively), were used to test the in vivo involvement of ADH with the oxidation of EGME into MAA. The toxicity of EGME in egg-to-adult and third instar larval-to-adult development is concentration and strain dependent. Higher detoxification occurs in the strain with increased ADH activity. EGME is much more toxic than its oxidation product MAA at the level of adult eclosion. Teratogenic effects were observed in the ADH-negative strain in spite of lacking ADH activity. EGME is apparently a teratogenic compound by itself.
Effect of Target Dynamics on Pharmacokinetics of a Novel Therapeutic Antibody against the Epidermal Growth Factor Receptor: Implications for the Mechanisms of Action (2006)

The epidermal growth factor receptor (EGFR) is overexpressed on many solid tumors and represents an attractive target for antibody therapy. Here, we describe the effect of receptor-mediated antibody internalization on the pharmacokinetics and dose-effect relationship of a therapeutic monoclonal antibody (mAb) against EGFR (2F8). This mAb was previously found therapeutically active in mouse tumor models by two dose-dependent mechanisms of action: blockade of ligand binding and induction of antibody-dependent cell-mediated cytotoxicity. In vitro studies showed 2F8 to be rapidly internalized by EGFR-overexpressing cells. In vivo, accelerated 2F8 clearance was observed in cynomolgus monkeys at low doses but not at high doses. This enhanced clearance seemed to be receptor dependent and was included in a pharmacokinetic model designed to explain its nonlinearity. Receptor-mediated clearance was also found to affect in situ antibody concentrations in tumor tissue. Ex vivo analyses of xenograft tumors of 2F8-treated nude mice revealed that relatively high antibody plasma concentrations were required for maximum EGFR saturation in high-EGFR-expressing human A431 tumors, in contrast to lower-EGFR-expressing human xenograft tumors. In summary, receptor-mediated antibody internalization and degradation provides a saturable route of clearance that significantly affects pharmacokinetics, particularly at low antibody doses. EGFR saturation in normal tissues does not predict saturation in tumor tissue as local antibody concentrations in EGFR-overexpressing tumors may be more rapidly reduced by antibody internalization. Consequently, antibody saturation of the receptor may be affected, thereby affecting the local mechanism of action.
Three-dimensional vision structure for robot applications (1988)

Focuses on the structure of robot sensing systems and the techniques for measuring and preprocessing 3-D data. To get the information required for controlling a given robot function, the sensing of 3-D objects is divided into four basic steps: transduction of relevant object properties (primarily geometric and photometric) into a signal; preprocessing the signal to improve it; extracting 3-D object features; and interpreting them. Each of these steps usually may be executed by several alternative techniques (tools). Tools for the transduction of 3-D data and data preprocessing are surveyed. The performance of each tool depends on the specific vision task and its environmental conditions, both of which are variable. Such a system includes so-called tool-boxes, one box for each sensing step, and a supervisor, which controls iterative sensing feedback loops and consists of a rule-based program generator and a program execution controller. Sensing step sequences and tools are illustrated for two 3-D vision applications at SRI International Company: visually guided robot arc welding and locating identical parts in a bin.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Androgen replacement therapy in women: myths and realities. (1997)

In recent years, much attention has been directed at the potential of androgen replacement in the menopausal woman. Testosterone (T) replacement, in various forms, is widely used. However, evidence is lacking for a profound T deficiency state with natural menopause. Data confirming efficacy are also scant, and side effects have been demonstrated with prolonged therapy. The adrenal androgens, dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEA-S), also in contradistinction to T, decline substantially with age. Preliminary studies involving replacement of physiologic levels of DHEA have demonstrated some potential benefits: enhancement of the immune system and enhancement of the growth hormone axis. However, long-term trials have not been performed to date, so this modality of androgen replacement remains in the realm of clinical investigation. Ovarian and adrenal androgen replacement in menopausal women, while theoretically appealing, remains imperfect to date and should be used judiciously, if at all.
High dose immunoglobulin therapy in severe juvenile chronic arthritis: long-term follow-up in 16 patients. (1991)

Sixteen children with severe juvenile chronic arthritis received high dose intravenous immunoglobulin (IVGG). Extra-articular symptoms improved to some degree in 6 of ten patients. A decrease in the number of active joints occurred in 7 patients of the 11 who received more than ten months of IVGG. Hemoglobin levels increased, the ESR and platelet counts decreased and the IgG levels diminished in most of the patients who received long term treatment. The treatment was totally ineffective in three children who had very severe disease. Two children had respectively a vasculitic rash and urticaria thought to be side effects of the treatment. One had proteinuria. This last might have been due to other therapeutic agents given. Although clinical and biological benefits occurred in some, the state of the patients who had short term (m = 2-3 months) or long term (m = 2-7 years) therapy was not different at the last visit.
NH-1,2,3-Triazoles from Azidomethyl Pivalate and Carbamates: Base-Labile N-Protecting Groups (2005)

NH-1,2,3-triazoles have been prepared via the copper(I)-catalyzed 1,3-dipolar cycloaddition between terminal alkynes and three N-protected organic azides, azidomethyl pivalate, azido­methyl morpholine-4-carboxylate, and azidomethyl N,N-diethylcarbamate. These organic azides were easily prepared on 0.1-mol scale in one or two steps from inexpensive commercially available materials. The cleaving properties of N-substituents in the resulting 1,2,3-triazole products with aqueous sodium hydroxide vary from <10 minutes at room temperature in the case of N-methyl pivalate, to 24 hours at room temperature in the case of N-methyl morpholine-4-carboxylate, to 24 hours at 85 °C in the case of N-methyl ­diethylcarbamate.
Ethanol increases the expression of functional delta-opioid receptors in neuroblastoma x glioma NG108-15 hybrid cells. (1986)

Ethanol inhibits opioid peptide binding to the delta-opioid receptor. When neuroblastoma x glioma NG108-15 hybrid cells are grown with 25-200 mM ethanol, opioid receptor density increases up to 2-fold without a change in receptor affinity. Since changes in neurotransmitter receptor density may be important in neuronal adaptations to ethanol, we investigated the underlying mechanisms and functional consequences of this phenomenon. The opiate antagonist, naloxone, also increased opioid receptor number, but produced a smaller effect than ethanol with greater fractional inhibition of binding; long term enhancement of binding by ethanol is therefore not a simple function of acute receptor inhibition. Ethanol did not inhibit receptor down-regulation by etorphine, an opiate agonist, and therefore is not likely to increase receptor expression through interference with tonic down-regulation by endogenous opioid peptides. Ethanol increased opioid receptor expression in NG108-15 cells treated with actinomycin D, but not cycloheximide; hence, normal protein synthesis, but not DNA transcription, may be required for this response. The opioid receptors induced in ethanol-treated cells were subject to normal up-regulation by naloxone, down-regulation by etorphine, and acute inhibition of agonist binding by Na+. Etorphine maximally inhibits cyclic AMP accumulation in NG108-15 cells with only fractional occupancy of opioid receptors. Chronic ethanol exposure increased the receptor reserve for this response, resulting in a 3.5-fold increase in the potency of etorphine for inhibiting phenylisopropyladenosine-stimulated cyclic AMP accumulation. Neuronal adaptation to ethanol may involve changes in the density of receptors that regulate cellular levels of cyclic AMP.