gebhart/patrepeval huggingface dataset:
Pharmacological and clinical properties of beraprost sodium, orally active prostacyclin analogue. (2001)

Prostacyclin is an endogeneous eicosanoid synthesized by vascular endothelial cells, and has potent inhibitory effects on platelet adhesion/aggregation and vasoconstriction. However, its therapeutic use is restricted by its extremely short half-life. Beraprost sodium (beraprost) is the first orally active prostacyclin analogue developed by TORAY Industries, Inc. Beraprost possesses a phenol moiety instead of the exo-enol ether moiety, which is the cause of the instability of prostacyclin, and has a modified omega-side chain that contributes to dissociating antiplatelet action from adverse reactions. In 1992, beraprost was approved as a drug for chronic arterial occlusion. Beraprost is now widely used clinically as "Dorner" or "Procylin". The indication for "primary pulmonary hypertension" was also approved in 1999. Recently in Europe, a placebo controlled trial named "Beraprost et Claudication Intermittent-2 (BERCI-2)" was performed, and it was reported that beraprost improved the walking distances of the patients. Beraprost has a variety of biological activities such as antiplatelet effects, vasodilation effects, antiproliferative effects on vascular smooth muscle cells, cytoprotective effects on endothelial cells and inhibitory effects on the production of inflammatory cytokines. On the basis of basic and clinical research, it has been suggested that beraprost is also effective for many intractable diseases. We expect that the relationship between reduced prostacyclin level and these diseases would be clarified and the beneficial effects of beraprost would be demonstrated by controlled clinical trials in the future.
Surgical simulation using virtual reality technology: design, implementation, and implications. (1994)

Atremendous demand exists for enhancing the way by which physicians learn new invasive procedures. Appropriate education in new medical and surgical procedures is often outpaced by the desire of physicians to incorporate a procedure in their practice. Computerized surgical simulations have the potential for improving surgical morbidy and mortality. Studies have shown that, for a wide range of diagnostic and therapeutic procedures, doctors doing their first few to several dozen cases are much more likely to make a greater number of errors. This phenomenon has been referred to as 'the learning curve'. Adequate proctoring of learners by experienced surgeons is cumbersome, as there are few surgeons experienced to proctor their colleagues. It is difficult for physicians, particularly those in rural areas, to travel to larger medical centers for training. The requirement also places a burden on experts who could become overwhelmed with proctoring requests, in addition to leaving their clinical responsibilities.
Members of the nuclear receptor superfamily regulate transcription from the hepatitis B virus nucleocapsid promoter (1997)

The role of members of the nuclear receptor superfamily of transcription factors in regulating hepatitis B virus (HBV) transcription was investigated. Hepatocyte nuclear factor 4 (HNF4), the retinoid X receptor (RXR), and the peroxisome proliferator-activated receptor (PPAR) were examined for their capacity to modulate the level of transcriptional activity from the four HBV promoters by transient-transfection analysis in the dedifferentiated hepatoma cell line, HepG2.1. It was found that the nucleocapsid and large surface antigen promoters were transactivated in the presence of HNF4 whereas the enhancer I/X gene, nucleocapsid, and large surface antigen promoters were transactivated in the presence of RXR and PPAR. Characterization of the nuclear receptors interacting with the nucleocapsid promoter region demonstrated that HNF4 is the primary transcription factor binding to the regulatory region spanning nucleotides -127 to -102 whereas HNF4, RXR-PPAR heterodimers, COUPTF1, and ARP1 bind the regulatory region spanning nucleotides -34 to -7. Transcriptional transactivation from the nucleocapsid promoter by HNF4 appears to be mediated through the two HNF4 binding sites in the promoter, whereas modulation of the level of transcription from the nucleocapsid promoter by RXR-PPAR appears to be regulated by the regulatory sequence element spanning nucleotides -34 to -7 and the HBV enhancer 1 region. These observations indicate that HBV transcription, and pregenomic RNA synthesis in particular, is regulated by ligand-dependent nuclear receptors. Agonists and antagonists capable of regulating the activity of these nuclear receptors may permit the modulation of HBV transcription and consequently replication during viral infection.
Morphology and Raman scattering spectrum of GaN nanowires embedded in nanochannels of template (2002)

The hexagonal wurtzite GaN nanowires embedded in the nanochannels of anodic alumina membrane were achieved by the direct reaction of Ga vapour with a constant flowing ammonia atmosphere. X-ray diffraction (XRD), scanning electron microscopy and transmission electron microscopy were used to measure the size and structures of the samples. The Raman scattering spectrum of ordered GaN nanowires was studied. The Raman spectrum of the GaN nanowire arrays is consistent with the hexagonal wurtzite structure GaN, in agreement with XRD observation. The E2(high), E1(TO), and A1(TO) phonon frequencies at 563, 553, and 529 cm-1 show the low-energy shifts, respectively. The shifts and band broadening of the Raman modes result from the nanosize effect.
Parametric polariton scattering in microresonators with three-dimensional optical confinement (2001)

Parametric scattering in square shaped microcavities that exhibit a three-dimensional confinement of light has been observed under resonant continuous wave excitation. The three lowest lying modes in the optical mode spectrum of these resonators are equidistantly spaced in energy. When resonantly exciting the middle mode parametric scattering into the ground and the second excited mode is observed. This process conserves energy, but conservation of momentum is not required, due to the breakdown of the translation invariance.
Road recognition from multifocal vision (2005)

The system for visual autonomous vehicle guidance which has been developed at UniBwM, has been installed into VaMoRs-P, a Mercedes 500 SEL sedan passenger car. To meet the requirements implicated by high cruising speed (up to 130 km/h) and low camera position, some changes in the design of the road detection and tracking algorithms had to be implemented. For robust visual road tracking and for reliable estimation vehicle position and heading parameters as well as of the road course, the maximal look-ahead range must be about 100 m. The 4D approach for estimation of the vehicle ego-state and the road course parameters by Kalman-filter techniques has been extended to a road model which is segmented into sections. These segments are modelled to be locally fixed, which leads to a better separation of the vehicle's ego-motion and the road course dynamics. Rearward viewing has been added to the already existing bifocal forward vision. In this paper, the basic concepts of the road recognition module are introduced and discussed.
In Vitro Evaluation of Viability, Integrity, and Inflammation in Genital Epithelia upon Exposure to Pharmaceutical Excipients and Candidate Microbicides (2010)

The use of microbicides is a promising approach for the prevention of HIV-1 transmission. Unfortunately, various candidates failed in clinical trials. In some cases, the candidate microbicide even resulted in enhanced virus transmission. Therefore, there is an urgent need to develop more predictive preclinical strategies to anticipate the in vivo efficiency/toxicity rate, including in vitro assays that evaluate effects on epithelial integrity and inflammation. The present study aims to identify potential safety issues concerning the use of microbicides and excipients commonly used in vaginal microbicide preparations. The toxicities of various active pharmaceutical ingredients (APIs; TMC-120, UC-781, tenofovir [PMPA], PRO-2000, and glycerol monolaurate [GML]) and excipients (preservatives, cosolvents, surfactants, and cyclodextrins) were evaluated using an in vitro dual-chamber model and uterine cervical explants. Epithelial viability and permeation of fluorescent virus-sized beads, as well as induction of interleukin-8 (IL-8; as a sensitive marker of an inflammatory response), were assessed. Surprisingly, cell viability and epithelial layer integrity were compromised by most excipients at concentrations near the typical concentration used in vaginal gels, and a significant increase in the production of IL-8 was observed at subtoxic concentrations. Within the APIs, TMC-120, UC-781, and PMPA showed higher selectivity indices than PRO-2000 and GML. In conclusion, identification of safety issues concerning the use of pharmaceutical excipients could help to formulate less toxic vaginal microbicide preparations.
Distance measures for effective clustering of ARIMA time-series (2002)

Much environmental and socioeconomic time-series data can be adequately modeled using autoregressive integrated moving average (ARIMA) models. We call such time series "ARIMA time series". We propose the use of the linear predictive coding (LPC) cepstrum for clustering ARIMA time series, by using the Euclidean distance between the LPC cepstra of two time series as their dissimilarity measure. We demonstrate that LPC cepstral coefficients have the desired features for accurate clustering and efficient indexing of ARIMA time series. For example, just a few LPC cepstral coefficients are sufficient in order to discriminate between time series that are modeled by different ARIMA models. In fact, this approach requires fewer coefficients than traditional approaches, such as DFT (discrete Fourier transform) and DWT (discrete wavelet transform). The proposed distance measure can be used for measuring the similarity between different ARIMA models as well. We cluster ARIMA time series using the "partition around medoids" method with various similarity measures. We present experimental results demonstrating that, using the proposed measure, we achieve significantly better clusterings of ARIMA time series data as compared to clusterings obtained by using other traditional similarity measures, such as DFT, DWT, PCA (principal component analysis), etc. Experiments were performed both on simulated and real data.
Design, Analysis, And Experimental Results For The Wobble Motor: An Eccentric-Motion Electrostatic Microactuator (1989)

A description is given of the design, fabrication and analysis of an electrostatically-driven microactuator in which a planetary-motion rotor rolls inside a cylindrically shaped stator cavity. The design has four primary advantages: (1) the motor geometry and the rolling motion enable very small gaps which are accurate and stable, and across which electrostatic forces act, leading to high forces on the rotor, (2) relative motion is achieved by rolling rather than sliding, thus obviating the concern over internal friction, (3) higher output torques can be traded for lower rotor speeds, due to immediate planetary reduction, and (4) the power output should be higher than for systems constructed using two-dimensional silicon fabrication approaches, since wobble motor lengths are not limited by such fabrication methods. The stator segment recruitment logic can range from simple, open-loop stepping to full servo-controlled commutation using rotor position sensors. Two-dimensional analytical and finite-element simulations which estimate motor torque generated by electrostatic fields have been used to determine the influence of: (1) rotor and stator radii, (2) stator segment angular width and position with respect to the contact point, (3) stator segment voltage(s), and (4) dielectric properties and dimensions (e.g., insulator thickness on rotor) of motor materials. Dynamic models of motor behavior are also under development. A number of eccentric-motion micro motors, constructed via different fabrication techniques, have been operated. Electro-discharge machining (EDM) is the fabrication method of choice for the prototypes presently used for experimental studies. Typical rotor diameters for the EDM motor are about 500 microns, with lengths of 5,000 microns. Motor operation has been achieved with commutation rates in excess of 120,000 RPM.
Potent, Selective, Orally Active 3-Oxo-1,4-benzodiazepine GPIIb/IIIa Integrin Antagonists (1996)

ADVERTISEMENT RETURN TO ISSUELetterNEXTPotent, Selective, Orally Active 3-Oxo-1,4-benzodiazepine GPIIb/IIIa Integrin AntagonistsJames M. Samanen, Fadia E. Ali, Linda S. Barton, William E. Bondinell, Joelle L. Burgess, James F. Callahan, Raul R. Calvo, Wenting Chen, Lichong Chen, Karl Erhard, Giora Feuerstein, Richard Heys, Shing-Mei Hwang, Dalia R. Jakas, Richard M. Keenan, Thomas W. Ku, Chet Kwon, Chao-Pin Lee, William H. Miller, Kenneth A. Newlander, Andrew Nichols, Michael Parker, Catherine E. Peishoff, Gerald Rhodes, Steven Ross, Arthur Shu, Richard Simpson, Dennis Takata, Tobias O. Yellin, Irene Uzsinskas, Joseph W. Venslavsky, Chuan-Kui Yuan, and William F. HuffmanView Author Information Department of Medicinal Chemistry, Radiochemistry Department, Department of Cellular Biochemistry, Pharmaceutical Sciences, Pharmacology Department, Department of Physical/Structural Chemistry, and Department of Pharmacokinetics, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406Cite this: J. Med. Chem. 1996, 39, 25, 4867–4870Publication Date (Web):December 6, 1996Publication History Received29 July 1996Published online6 December 1996Published inissue 1 January 1996https://pubs.acs.org/doi/10.1021/jm960558ahttps://doi.org/10.1021/jm960558arapid-communicationACS PublicationsCopyright © 1996 American Chemical SocietyRequest reuse permissionsArticle Views431Altmetric-Citations61LEARN 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:Aggregation,Antagonists,Cells,Peptides and proteins,Receptors Get e-Alerts
Observation of narrow-band Si L-edge Čerenkov radiation generated by 5 MeV electrons (2001)

Narrow-band Čerenkov radiation at 99.7 eV has been generated by 5 MeV electrons in a silicon foil, with a yield ∼1×10−3 photon/electron. These measurements demonstrate the feasibility of a compact, narrow-band, and intense soft x-ray source based on small electron accelerators. The observed yield and dependence of the photon spectrum on emission angle are in agreement with theoretical predictions for Čerenkov radiation based on refractive index data of silicon.
Yeast proteins related to the p40/laminin receptor precursor are required for 20S ribosomal RNA processing and the maturation of 40S ribosomal subunits. (1999)

Numerous studies have linked the overexpression of the Mr 37,000 laminin receptor precursor (37-LRP) to tumor cell growth and proliferation. The role of this protein in carcinogenesis is generally considered in the context of its putative role as a precursor for the Mr 67,000 high-affinity laminin receptor. Recent studies have shown that 37-LRP, also termed p40, is a component of the small ribosomal subunit indicating that it may be a multifunctional protein. The p40/37-LRP protein is highly conserved phylogenetically, and closely related proteins have been identified in species as evolutionarily distant as humans and the yeast, Saccharomyces cerevisiae. Yeast homologues of p40/37-LRP are encoded by a duplicated pair of genes, RPS0A and RPS0B. The Rps0 proteins are essential components of the 40S ribosomal subunit. Previous results have shown that cells disrupted in either of the RPS0 genes have a reduction in growth rate and reduced amounts of 40S ribosomal subunits relative to wild-type cells. Here, we show that the Rps0 proteins are required for the processing of the 20S rRNA-precursor to mature 18S rRNA, a late step in the maturation of 40S ribosomal subunits. Immature subunits that are depleted of Rps0 protein that contain the 20S rRNA precursor are preferentially excluded from polysomes, which indicates that their activity in protein synthesis is dramatically reduced relative to mature 40S ribosomal subunits. These data demonstrate that the assembly of Rps0 proteins into immature 40S subunits and the subsequent processing of 20S rRNA represent critical steps in defining the translational capacity of yeast cells. If the function of these yeast proteins is representative of other members of the p40/37-LRP family of proteins, then the role of these proteins as key components of the protein synthetic machinery should also be considered as a basis for the linkage between the their overexpression and tumor cell growth and proliferation.
whitesnake/sfpq is required for cell survival and neuronal development in the zebrafish (2007)

Organogenesis involves both the development of specific cell types and their organization into a functional three-dimensional structure. We are using the zebrafish to assess the genetic basis for brain organogenesis. We show that the whitesnake mutant corresponds to the sfpq (splicing factor, proline/glutamine rich) gene, encoding the PSF protein (polypyrimidine tract-binding protein-associated splicing factor). In vitro studies have shown that PSF is important for RNA splicing and transcription and is a candidate brain-specific splicing factor, however, the in vivo function of this gene is unclear. sfpq is expressed throughout development and in the adult zebrafish, with strong expression in the developing brain, particularly in regions enriched for neuronal progenitors. In the whitesnake mutant, a brain phenotype is visible by 28 hr after fertilization, when it becomes apparent that the midbrain and hindbrain are abnormally shaped. Neural crest, heart, and muscle development or function is also abnormal. sfpq function appears to be required in two distinct phases during development. First, loss of sfpq gene function leads to increased cell death throughout the early embryo, suggesting that cell survival requires functional PSF protein. Second, sfpq function is required for differentiation, but not for determination, of specific classes of brain neurons. These data indicate that, in vertebrates, sfpq plays a key role in neuronal development and is essential for normal brain development.
Systemic Adenosine Infusion Alleviates Spontaneous and Stimulus Evoked Pain in Patients with Peripheral Neuropathic Pain (1995)

In seven patients with peripheral neuropathic pain, the effect of systemic adenosine infusion on pain symptoms was evaluated in a double-blind, placebo controlled, cross-over study. The study infusions, adenosine (50 micro gram centered dot kg-1 centered dot min-1) or placebo, were given intravenously (IV) during 45-60 min at two separate occasions. Before and during infusions, bedside examination of sensibility and quantitative sensory testing (QST), i.e., assessments of perception thresholds for touch, touch-evoked pain, cold, warmth, painful heat, and cold, were performed. In the neuropathic area, sensation magnitude was rated by a visual analog scale (100 mm VAS) using a pin and at perception threshold for touch-evoked pain using von Frey filaments. Adenosine infusion reduced spontaneous pain (P < 0.05), and caused an increase of the touch-evoked pain threshold from 10.8 +/- 5.3 to 22.2 +/- 6.9 g (P < 0.05), whereas placebo had no effect. Pain intensity at perception threshold for touch-evoked pain was, however, unaltered. Pinprick-evoked pain in the neuropathic areas was reduced from 53 +/- 11 to 29 +/- 10 mm (P < 0.05). No other sensory modality was consistently changed during adenosine infusion. In conclusion, the present study demonstrates that adenosine infusion alleviates spontaneous neuropathic pain, tactile allodynia, and pinprick hyperalgesia in patients with peripheral neuropathic disorders, probably by a central mechanism of action. (Anesth Analg 1995;81:713-7)
Synthesis and reactions of N-protected 2-lithiated pyrroles and indoles. The tert-butoxycarbonyl substituent as a protecting group (1981)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis and reactions of N-protected 2-lithiated pyrroles and indoles. The tert-butoxycarbonyl substituent as a protecting groupIltifat Hasan, Edmund R. Marinelli, Li-Ching Chang Lin, Frank W. Fowler, and Alan B. LevyCite this: J. Org. Chem. 1981, 46, 1, 157–164Publication Date (Print):January 1, 1981Publication History Published online1 May 2002Published inissue 1 January 1981https://pubs.acs.org/doi/10.1021/jo00314a034https://doi.org/10.1021/jo00314a034research-articleACS PublicationsRequest reuse permissionsArticle Views3744Altmetric-Citations149LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Defects of cytochrome c oxidase in the substantia nigra of Parkinson's disease: An immunohistochemical and morphometric study (1997)

Defects of respiratory chain complexes were considered as possible pathogenetic mechanisms in Parkinson's disease (PD). Changes of cytochrome c oxidase (COX) in four different nuclei of the substantia nigra of 8 PD cases and 10 age-matched controls were investigated by means of morphometry and immunohistochemistry. Pigmented neurons with COX defects were randomly distributed within the the four nuclei of PD cases, but only in the posterolateral nucleus was the numerical density of pigmented neurons with COX defects significantly increased compared with controls. The numerical density of pigmented neurons without COX defects was significantly reduced in the anteromedial, anterointermediolateral, and posterolateral nuclei in PD. The cell size of pigmented neurons with and without COX defects was significantly diminished in the anteromedial and posterolateral nuclei of PD cases. It is suggested that complex IV defects in nigral neurons are most probably a result of accelerated aging, but are least likely to be a primary aspect of the pathogenetic processes occurring in PD.