gebhart/patrepeval huggingface dataset:
Selective .beta.3-adrenergic agonists of brown adipose tissue and thermogenesis. 2. [4-[2-[(2-Hydroxy-3-phenoxypropyl)amino]ethoxy]phenoxy]acetamides (1992)

The ester methyl [4-[2-[(2-hydroxy-3-phenoxypropyl)amino]ethoxy]phenoxy]acetate (1) (R1 = OMe) had previously been identified as the most interesting member of a series of selective beta 3-adrenergic agonists of brown adipose tissue and thermogenesis in the rat. In vivo it acts mainly via the related acid 1 (R1 = OH). Amides have been examined to determine whether they have advantages over the ester. In particular, in the rat and dog the half-lives of amides of appropriate potency were no longer than those of the ester. The amide (S)-4-[2-[(2-hydroxy-3-phenoxypropyl)amino]ethoxy]-N-(2- methoxyethyl)phenoxyacetamide [S-27, ICI D7114] was selected as having properties consistent with a sustained-release formulation should that prove necessary. Unlike the ester it is resistant to hydrolysis in the gut lumen. Further testing of ICI D7114 has shown that in the rat, cat, and dog it stimulates the beta 3-adrenergic receptor in brown adipose tissue at doses lower than those at which it affects beta 1- and beta 2-adrenergic receptors in other tissues. Slimming effects were observed in the dog. ICI D7114 may be a selective thermogenic agent in man and may be useful in the treatment of obesity and diabetes.
Trial and Error: Using Previous Experiences as Simulation Models in Humanoid Motor Learning (2016)

Since biological systems have the ability to efficiently reuse previous experiences to change their behavioral strategies to avoid enemies or find food, the number of required samples from real environments to improve behavioral policy is greatly reduced. Even for real robotic systems, it is desirable to use only a limited number of samples from real environments due to the limited durability of real systems to reduce the required time to improve control performance. In this article, we used previous experiences as environmental local models so that the movement policy of a humanoid robot can be efficiently improved with a limited number of samples from its real environment. We applied our proposed learning method to a real humanoid robot and successfully achieve two challenging control tasks. We applied our proposed learning approach to acquire a policy for a cart-pole swing-up task in a real-virtual hybrid task environment, where the robot waves a PlayStation (PS) Move motion controller to move a cart-pole in a virtual simulator. Furthermore, we applied our proposed method to a challenging basketball-shooting task in a real environment.
Monoclonal antibodies specific to the alpha-subunit of the mast cell's Fc epsilon R block IgE binding and trigger histamine release. (1987)

In an attempt to block the interactions between IgE and its receptor on mast cells (Fc epsilon R), we have established anti-Fc epsilon R monoclonal antibodies (mAb) by fusion of myeloma cells with mouse splenocytes immunized with irradiated rat basophilic leukemia (RBL) cells. Two anti-Fc epsilon R mAb were obtained (denoted 4.7 and 5.14) that could specifically bind to RBL and mast cells. This binding could be inhibited by IgE. The mAb and their F(ab')2 fragments inhibited 125I-IgE binding to RBL cell and triggered cell degranulation. The Fab' fragments, on the other hand, could only inhibit IgE binding but did not stimulate cell degranulation. Furthermore, these monovalent fragments inhibited RBL and mast cell degranulation induced by IgE-antigen complexes both in vitro and in vivo in the passive cutaneous anaphylaxis reaction. The number of mAb 4.7 and 5.14 molecules bound per RBL cells was similar to that of IgE; nevertheless, mAb 4.7 and 5.14 recognized different epitopes on the IgE receptor. Immunoprecipitation and immunoblotting analysis demonstrated that the mAb reacted with the alpha-subunit of the Fc epsilon R. Our findings establish the anti-Fc epsilon R mAb as a useful reagent for the isolation and characterization of the Fc epsilon R's alpha-subunit and the monomeric (Fab') for blocking the IgE-Fc epsilon R interactions.
Altered excitability of goldfish Mauthner cell following axotomy. II. Localization and ionic basis (1986)

The ionic basis and spatial localizations of spike generation were examined in normal and axotomized goldfish Mauthner (M-) cells using intra- and extracellular recordings and pharmacological manipulation of ionic conductances, including localized iontophoretic drug applications. Tetrodotoxin (TTX) abolished both the initial segment (IS) spike in normal cells and the larger, two-component action potential in axotomized cells, whereas calcium (Ca2+) blockers did not. Thus, sodium (Na+) appears to be the major inward current carrier in both cases. A shoulder or plateau following the fast-rising Na+-dependent action potential was unmasked in both normal and axotomized M-cells by intracellular injections of tetraethylammonium (TEA), either alone or in conjunction with 4-aminopyridine (4-AP) or cesium (Cs+). This plateau potential was abolished by superfusing with saline containing the Ca2 antagonists, Co2+, Mn2+, or Cd2+. However, barium (Ba2+), which normally substitutes for Ca2+ and also blocks K+ conductances, did not produce a plateau spike, and no action potentials could be evoked in the presence of TTX. Simultaneous extra- and intracellular recordings from the soma and lateral dendrite revealed that both the full-sized axotomized spike and its individual labile components were always maximal at the soma. These data support the earlier suggestion that the axotomy-induced electrogenicity is primarily localized to that region. Iontophoretic application of TTX inside the axon cap, a distinctive neuropil surrounding the initial segment and the axon hillock and circumscribed by a glial border, and at various positions along the lateral dendrite confirmed the Na+-dependency of the action potentials recorded in normal and axotomized cells and further demonstrated that the soma generates the additional spike component in the latter. The results suggest that axotomy causes a persistent change in voltage-gated Na+ channel distribution in the M-cell, with Na+ channels appearing or becoming more numerous in the soma while becoming less concentrated in the initial segment-axon hillock. Possible related shifts in other voltage-dependent conductances are also discussed. Finally, these are the first detailed studies of the ionic basis of axotomy-induced electrogenicity in a vertebrate neuron, central or peripheral, and the similarity to the results obtained with invertebrate neurons suggests common mechanisms underlying the axon reaction.
Circulating Endothelial Microparticles Are Associated with Vascular Dysfunction in Patients with End-Stage Renal Failure (2005)

Endothelial dysfunction and arterial stiffness are major determinants of cardiovascular risk in patients with end-stage renal failure (ESRF). Microparticles are membrane fragments shed from damaged or activated cells. Because microparticles can affect endothelial cells, this study investigated the relationship between circulating microparticles and arterial dysfunction in patients with ESRF and identified the cellular origin of microparticles associated with these alterations. Flow cytometry analysis of platelet-free plasma from 44 patients with ESRF indicated that circulating levels of Annexin V+ microparticles were increased compared with 32 healthy subjects, as were levels of microparticles derived from endothelial cells (three-fold), platelets (16.5-fold), and erythrocytes (1.6-fold). However, when arterial function was evaluated noninvasively in patients with ESRF, only endothelial microparticle levels correlated highly with loss of flow-mediated dilation (r = -0.543; P = 0.004), increased aortic pulse wave velocity (r = 0.642, P < 0.0001), and increased common carotid artery augmentation index (r = 0.463, P = 0.0017), whereas platelet-derived, erythrocyte-derived, and Annexin V+ microparticle levels did not. In vitro, microparticles from patients with ESRF impaired endothelium-dependent relaxations and cyclic guanosine monophosphate generation, whereas microparticles from healthy subjects did not. Moreover, in vitro endothelial dysfunction correlated with endothelial-derived (r = 0.891; P = 0.003) but not platelet-derived microparticle concentrations. In fact, endothelial microparticles alone decreased endothelial nitric oxide release by 59 +/- 7% (P = 0.025). This study suggests that circulating microparticles of endothelial origin are tightly associated with endothelial dysfunction and arterial dysfunction in ESRF.
Ultraviolet–Visible Chiroptical Activity of Aluminum Nanostructures (2017)

Ultraviolet (UV)-resonant metals (e.g., aluminum) typically have low melting point to cause a fabrication difficulty in helical sculpture to generate plasmons with chiroptical activity in the UV region. In this work, using glancing angle deposition (GLAD), two new methods are devised to generate crystalline chiral Al nanostructures that have stable chiroptical response in the UV-visible region originating from intrinsic helical structures. One approach involves fast substrate rotation during GLAD to fabricate Al nanoparticles (AlNPs) with hidden helicity; another is to deposit an achiral Al thin film on a host of plasmonic chiral NPs, such that the helical structures are duplicated from the chiral host to the achiral guest of Al nanocappings. The host@guest helicity duplication is a new GLAD methodology to generate chiroptically active plasmons, which can be generally adapted to diverse plasmonic metals for tailoring plasmonic chiroptical activity flexibly in the UV-visible region. More importantly, this work offers those two new methods to generate UV-active plasmonic chiral substrates, which can markedly enhance chiroptical activity of biomolecules. It would open a door to develop surface-enhanced chiroptical spectroscopies for sensitively monitoring stereobiochemical information, which is of prominent interest in understanding a wide range of homochirality-determined biological phenomena.
An imaging device that uses the wavelet transformation as the image reconstruction algorithm (1992)

Abstract Many imaging devices have been constructed that use fourier transform techniques for image reconstruction as well as for image analysis. The basis functions in the fourier transform space are sinusoids. These are not localized. Therefore it should not be expected that highly localized behavior of a signal be characterized well using functions distributed evenly throughout the interval of the integral transform. Also, the phase cancellations of a conventional impulse signal are not handled well by fourier techniques. On the other hand, the basis functions of the wavelet transformation are highly localized, i.e., these exhibit compact support, yet are orthonormal. The multispectral decomposition algorithm of the wavelet transformation is used to analyze the signal returning from the reflections of a single ultrasonic transducer with a focused beam and operated in the focal zone. The choice of frequency depends upon the mutually antagonistic factors of penetration (α f –2 ) and resolution (α f ). The signal sent into the sample should not be the impulse response signal used in conventional devices; rather, it should be a time‐reversed replica of a single or a linear combination of the most highly localized basis function wavelets. The returning signal is a sequence of translates of the wavelets plus perhaps some lower‐resolution wavelets. The translations are proportational to the time of flight of the signal. The wavelet transformation is superb at discriminating the population of each of these translates which is identically the A‐scan signal. The transmitted signal, which is a time‐reversed single wavelet or a linear combination of wavelets, is not easy to produce. Inexpensive ultrasound transducers have resonances which make it difficult to produce any desired wave form. Wavelet shape is far from arbitrary. Precise wave shaping is performed by measuring the impulse response function of the transducer; then, the desired wave shape is convolved with the inverse of the measured impulse response function of the transducer. This produces the signal to be presented to the pulse generation circuit. Care is taken to damp the impulse response so that there are no zeros. The received signal is sampled at an even rate which is carefully chosen to match the time delay of one wavelet translate to the next. B‐scan, C‐scan, and volume imaging are easily accomplished using a sequence of A‐scan data, all by conventional techniques. A single A‐scan requires less than 2 ms to perform and reconstruct with a high‐speed arithmetic unit which was designed in conjunction with this work and is now commercially available.
The new paradigm in the treatment of colorectal cancer: are we hitting the right target? (2007)

The treatment of advanced colorectal cancer has definitely advanced in the last 10 years as newer and more active cytotoxic chemotherapy agents have become available. Better understanding of different fundamental molecular changes in carcinogenesis has resulted in the emergence of important therapeutic targets in colon cancer treatment. The era of nihilism has been replaced by a time of optimism with the development of targeted therapy, with the promise of agents with improved activity and a better toxicity profile in the management of colon cancer. This review focuses on novel agents, particularly targeted therapy in both earlier and more advanced phases of clinical investigations.
Study of relative quantification of Tc-99m with partial volume effect and spillover correction for SPECT oncology imaging (2005)

The apparent concentration of activity in nuclear medicine images is altered by the finite spatial resolution of the imaging systems blurring the counts emitted at a given site out into a surrounding volume in the reconstructed slices. If a structure only partially occupies this volume then more counts will be lost from the location then are brought back in to it from activity within the structure. This is the partial volume effect (PVE). Similarly, counts from surrounding structures can be blurred into the structure. This spillover (SO) also alters the apparent concentration of activity. In total these effects alter the detection and quantification of activity within structures. The increased availability of dual-modality imaging systems whereby high-resolution anatomical information which is registered with the emission slices makes this anatomical information available for use in correcting for the PVE and SO. In this study we investigated the use a template projection-reconstruction method for correction PVE and SO in terms of both its impact of visual image quality and the quantification of activity in simulated spheres of varying contrast relative to a uniform background distribution of activity. We determined that such corrections can dramatically improve both the visualization and quantification of activity within the spheres
Shift in AP-2α localization characterizes astrocytoma progression (2007)

Activator protein 2alpha (AP-2alpha) has been shown to be lost in the advanced stages of many cancers, including gliomas. In this study, we wanted to analyze the expression of AP-2alpha in astrocytoma samples of different grades both at the RNA level, by real-time qPCR and at the protein level, by immunohistochemistry, and to examine its correlation, if any, with patient outcome. Five Grade I, 14 Grade II, 18 Grade III, 72 Grade IV samples and 13 normal brain controls were included. We did not find any clear pattern of regulation at the RNA level with tumor grade. The RNA expression levels however, correlated to a large extent with the nuclear AP-2alpha staining in these samples (72.09%; 31/43). Further, we did not find a complete loss of nuclear AP-2alpha expression in the higher grades, in contrast to previous reports. Interestingly, we found cytoplasmic AP-2alpha expression in a majority of higher grade astrocytomas (Grade IV-85%; 33/39 and Grade III-74%; 14/19) in comparison to lower grades (Grade I-0%; 0/5 and Grade II-37.5%; 3/8) suggesting that the translocation of this protein from the nucleus to the cytoplasm may be responsible for the increased malignancy. The nuclear expression in these grades was found to be concomitantly reduced. Within GBMs, we found that decreased nuclear expression was indicative of a better prognosis. The striking observation was the shift in localization of this protein from the nucleus to the cytoplasm with increasing tumor grade, pointing to a crucial role for this transcription factor in the progression of astrocytomas.
A stable feedback control of the buffer state using the controlled Lagrange multiplier method (1994)

We propose a stable feedback control algorithm of the buffer state using the controlled Lagrange multiplier in combined rate-distortion characteristics for a buffer-constrained adaptive quantization. The proposed algorithm is established using feedback control theory and is described by the state equation with nonlinearity in the feedback path. The nonlinearity of the state equation comes from the average distortion-rate curve of the information source. The stability of this buffer control algorithm is shown using Lyapunov stability theory. It is shown that the stability of the algorithm depends on average distortion-rate curve and buffer size, and sufficient conditions for the algorithm to be stable are obtained from the usual average distortion-rate curve. In addition, it is observed from experimental results that the performance of the proposed algorithm and the optimal algorithm is not significantly different. Although the proposed algorithm does not provide optimal performance, the algorithm can be implemented easily with quite low computational complexity, as compared with others.
The Displacement of Aromatic Substituents by Halogen Atoms<sup>1</sup> (1957)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTThe Displacement of Aromatic Substituents by Halogen Atoms1Bernard Miller and Cheves WallingCite this: J. Am. Chem. Soc. 1957, 79, 15, 4187–4191Publication Date (Print):August 1, 1957Publication History Published online1 May 2002Published inissue 1 August 1957https://pubs.acs.org/doi/10.1021/ja01572a054https://doi.org/10.1021/ja01572a054research-articleACS PublicationsRequest reuse permissionsArticle Views262Altmetric-Citations34LEARN 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
Mechanism of stereospecific production of L-amino acids from the corresponding 5-substituted hydantoins by Bacillus brevis. (1988)

The mechanism of Stereospecific production of L-amino acids from the corresponding 5-substituted hydantoins by Bacillus brevis AJ-12299 was studied. The enzymes involved in the reaction were partially purified by DEAE-Toyopearl 650M column chromatography and their properties were investigated. The conversion of DL-5-substituted hydantoins to the corresponding L-amino acids consisted of the following two successive reactions. The first step was the ring-opening hydrolysis to N-carbamoyl amino acids catalyzed by an ATP dependent L-5-substituted hydantoin hydrolase. This reaction was Stereospecific and the N-carbamoyl amino acid produced was exclusively the L-forrn. N-Carbamoyl-L-amino acid was also produced from the D-form of 5-substituted hydantoin, which suggests that spontaneous racemization occurred in the reaction mixture. In the second step, N-carbamoyl-L-amino acid was hydrolyzed to L-amino acid by an N-carbamoyl-L-amino acid hydrolase, which was also an L-specific enzyme. The ATP dependency of the L-5-substituted hydantoin hydrolase was supposed to be the limiting factor in the production of L-amino acids from the corresponding 5-substituted hydantoins by this bacterium.
Some Biologic Characteristics of Transplantable Lines of Mouse Adenocarcinomas of the Colon<xref ref-type="fn" rid="FN2">2</xref><xref ref-type="fn" rid="FN3">3</xref> (1980)

During a 5-year period colon tumors induced by 1,2-dimethylhydrazine dihydrochloride treatment in NMRI mice were transplanted sc into isologous mice to obtain transplantable tumor lines that might serve as experimental models for human colon cancer. The resultant 17 serially transplantable tumor lines were adenocarcinomas varying in degree of differentiation and mucin production. Two of the lines passaged for 5 years and used in chemotherapy studies have shown histologic progression toward dedifferentiation with concomitant acceleration of growth rate.
<i>Nicotiana</i> (<i>Nicotiana tobaccum, Nicotiana benthamiana</i>) (2006)

Agrobacterium-mediated transformation of Nicotiana species, namely, Nicotiana tobaccum and Nicotiana benthamiana, using leaf disks as the target explant has provided the plant community with a valuable tool for rapid evaluation of transgenes in higher plants. This protocol has a number of desirable attributes: readily available explant material, high efficiency, and a relatively quick turnaround time. The in vitro regeneration scheme of the leaf disks is prolific and follows an indirect organogenic differentiation. N. tobaccum and N. benthamiana are highly susceptible to a variety of disarmed A. tumefaciens strains, and the transformation system is amenable to a number of selection agents. This protocol has proved to be easily transferable to a point at which a single investigator with minimal training can generate thousand of events per year. Moreover, seed size and quantity per event permit monitoring of segregation in Petri plates, and sufficient biomass can be accrued from an individual plant, which can be either clonally propagated or allowed to self-pollinate or easily outcrossed.
A diffusion theory model of spatially resolved, steady-state diffuse reflectance for the noninvasive determination of tissue optical properties <i>in</i> <i>vivo</i> (1992)

A model based upon steady-state diffusion theory which describes the radial dependence of diffuse reflectance of light from tissues is developed. This model incorporates a photon dipole source in order to satisfy the tissue boundary conditions and is suitable for either refractive index matched or mismatched surfaces. The predictions of the model were compared with Monte Carlo simulations as well as experimental measurements made with tissue simulating phantoms. The model describes the reflectance data accurately to radial distances as small as 0.5 mm when compared to Monte Carlo simulations and agrees with experimental measurements to distances as small as 1 mm. A nonlinear least-squares fitting procedure has been used to determine the tissue optical properties from the radial reflectance data in both phantoms and tissues in vivo. The optical properties derived for the phantoms are within 5%-10% of those determined by other established techniques. The in vivo values are also consistent with those reported by other investigators.