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1.
In an experiment designed to distinguish between the behavioral consequences of treatment with SCH-23390, a D1 dopamine receptor blocker, and raclopride, a D2 antagonist, rats were trained to perform a water-reinforced forelimb operant response. Response rate and the duration of each forelimb contact with the operandum were recorded. In addition, the durations of the rat's visits to the reward well were detected by a photobeam which was blocked by the rat's muzzle as it remained at the reward well. In a between-groups dosing design, separate groups of rats (11-13 rats/group) received SCH-23390 (0, 0.01, 0.02, 0.04, 0.08, 0.12 mg/kg, IP, 30 min) or raclopride (0. 0.05, 0.1, 0.2, 0.4, 0.8 mg/kg, IP, 30 min) for 21 consecutive days. Quantitative analyses indicated that for comparable amounts of operant rate reduction, raclopride had a significantly greater tendency than SCH-23390 to increase the duration of operant responses and to increase the maximum muzzle entry duration (i.e., to induce microcatalepsy). The results support the idea that at relatively low doses D2 antagonism is more likely than D1 antagonism to produce effects identified preclinically with extrapyramidal side effects.  相似文献   
2.
Abstract

The main topic of this paper is the nondestructive inspection of adhesively bonded lap joints by using ultrasonic guided (plate) waves. A noncontact, couplant-free method that employs capacitive air-coupled transducers is demonstrated for the inspection of thin aluminum joints with dimensions typical of aircraft fuselage and wing panels. Two types of bond defects, disbonded regions and regions of poorly cured (low-cohesive-strength) adhesive, are successfully detected by measuring the amplitude decrease of selected plate waves leaking from one adherend to the other one through the bondline. It is shown that proper choice of the vibrating mode structure, in terms of cross-sectional displacement distributions, is needed in order to maximize the sensitivity of the inspection to the presence of the low-cohesive-strength bond.

Results from a dynamic photoelasticity study are also presented to visualize fundamental behavior of propagating plate waves and study their interaction with bond defects in glass lap joints. The photoelastic results confirm in a clear, pictorial manner certain assumptions on plate wave leakage through the bond, including the influence of vibrating mode structure on the detection of low-strength bonds.  相似文献   
3.
Boronic acids are known reversible covalent inhibitors of serine β-lactamases. The selectivity and high potency of specific boronates bearing an amide side chain that mimics the β-lactam's amide side chain have been advanced in several studies. Herein, we describe a new class of boronic acids in which the amide group is replaced by a bioisostere triazole. The boronic acids were obtained in a two-step synthesis that relies on the solid and versatile copper-catalyzed azide–alkyne cycloaddition (CuAAC) followed by boronate deprotection. All of the compounds show very good inhibition of the Klebsiella pneumoniae carbapenemase KPC-2, with Ki values ranging from 1 nM to 1 μM, and most of them are able to restore cefepime activity against K. pneumoniae harboring blaKPC-2. In particular, compound 1 e , bearing a sulfonamide substituted by a thiophene ring, proved to be an excellent KPC-2 inhibitor (Ki=30 nM); it restored cefepime susceptibility in KPC-Kpn cells (MIC=0.5 μg/mL) with values similar to that of vaborbactam (Ki=20 nM, MIC in KPC-Kpn 0.5 μg/mL). Our findings suggest that α-triazolylboronates might represent an effective scaffold for the treatment of KPC-mediated infections.  相似文献   
4.
The aim of this study was to compare high-resolution 2D TOF with high-resolution 3D TOF in the study of internal carotid artery disease. Sixty-four patients with clinical signs of cerebrovascular insufficiency were studied with a superconductive 1.5 T magnet using two techniques: 2D and 3D TOF. Digital subtraction angiography (DSA) was the gold standard. The 2D TOF technique was performed using the following parameters: TR/TE/FA/MA 49 ms/9 ms/60 degrees/512 x 256; the 3D TOF was performed with the following parameters: TR/TE/FA/MA 50 ms/8 ms/20 degrees/512 x 256. The 2D TOF agreed with DSA in 116 of 128 diagnostic judgments (90%) and overestimated seven times. The 3D TOF technique agreed with DSA in 125 of 128 diagnostic judgments (97%) with one overestimation and two underestimations. There was no statistically significant difference (P < 0.05) between the two different techniques. Our study confirms the high reliability of the methodology carried out with the high-resolution 2D and 3D technique.  相似文献   
5.
Design and control of an IPMC wormlike robot.   总被引:2,自引:0,他引:2  
This paper presents an innovative wormlike robot controlled by cellular neural networks (CNNs) and made of an ionic polymer-metal composite (IPMC) self-actuated skeleton. The IPMC actuators, from which it is made of, are new materials that behave similarly to biological muscles. The idea that inspired the work is the possibility of using IPMCs to design autonomous moving structures. CNNs have already demonstrated their powerfulness as new structures for bio-inspired locomotion generation and control. The control scheme for the proposed IPMC moving structure is based on CNNs. The wormlike robot is totally made of IPMCs, and each actuator has to carry its own weight. All the actuators are connected together without using any other additional part, thereby constituting the robot structure itself. Worm locomotion is performed by bending the actuators sequentially from "tail" to "head," imitating the traveling wave observed in real-world undulatory locomotion. The activation signals are generated by a CNN. In the authors' opinion, the proposed strategy represents a promising solution in the field of autonomous and light structures that are capable of reconfiguring and moving in line with spatial-temporal dynamics generated by CNNs.  相似文献   
6.
Seventeen Leuconostoc mesenteroides and 33 Lactobacillus paracasei subsp. paracasei from traditional Pecorino di Filiano cheese were tested for their potential use as adjunct starters, and a study of their genetic variability was carried out. Forty one per cent (41%) of Leumesenteroides and 46% of Lb. paracasei subsp. paracasei showed medium–high proteolytic activity, while high lipolytic activity was detected in 18% of Lb. paracasei subsp. paracasei. The aminopeptidase activity of Lb. paracasei subsp. paracasei was higher than that of Leumesenteroides. Strain diversity by RAPD analysis showed a high degree of heterogeneity. This study identified strains with unusual properties that could be good candidates as adjuncts in a starter to manufacture PF cheese.  相似文献   
7.
A Candida albicans expression library was constructed from RNA isolated from regenerating protoplasts. A 1.4-kb cDNA clone was used to isolate a genomic fragment. Sequence analysis revealed an open reading frame of 593 amino acids with an overall identity of 63.6% with the phenylalanyl-tRNA synthetase beta subunit (FRS1) of Saccharomyces cerevisiae. We named it CaFRS1. It is located in a single copy in chromosome R, SfiI fragment M. Its expression showed a decrease during the cell wall regeneration process in protoplasts of both yeast and mycelial cells of C. albicans, suggesting its requirement thereof in initial steps of the cell wall synthesis.  相似文献   
8.
The use of macroporous monolithic matrices in the purification of biocompounds is constantly growing and developing. In this work, the objective was to optimize the quantity of N-acetyl-D-glucosamine (D-GlcNAc) immobilized on the surface of macroporous polymeric cryogels for capture of lectins from less clarified solutions. Surface response methodology was applied and it was observed that the immobilization temperature of the glutaraldehyde (GLU) and the D-GlcNAc concentration influenced the amount of sugar immobilized. The matrices produced with 1.1% of allyl glycidyl ether were functionalized by GLU. Optimal maximum condition was obtained with mean value of 160.39 ± 26.38 mg of D-GlcNAc immobilized per gram of dry cryogel. Characterization analyses of the matrices showed that the activation process was effective, maintaining the macroporous structure and physical characteristics. The adsorbents produced were tested for capture of lectins from a crude protein solution of barley. At tested conditions, adsorbent capture around 11% of protein in solution but reduce the hemaglutinating capacity in 40%, demonstrating its selectivity. The cryogels functionalized with D-GlcNAc present potential for use in capture compounds by affinity with carbohydrates, such as lectins. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019 , 136, 47956.  相似文献   
9.
Resveratrol (RSV) is a natural compound that displays several pharmacological properties, including anti-cancer actions. However, its clinical application is limited because of its low solubility and bioavailability. Here, the antiproliferative and anti-inflammatory activity of a series of phenylacetamide RSV derivatives has been evaluated in several cancer cell lines. These derivatives contain a monosubstituted aromatic ring that could mimic the RSV phenolic nucleus and a longer flexible chain that could confer a better stability and bioavailability than RSV. Using MTT assay, we demonstrated that most derivatives exerted antiproliferative effects in almost all of the cancer cell lines tested. Among them, derivative 2, that showed greater bioavailability than RSV, was the most active, particularly against estrogen receptor positive (ER+) MCF7 and estrogen receptor negative (ER-) MDA-MB231 breast cancer cell lines. Moreover, we demonstrated that these derivatives, particularly derivative 2, were able to inhibit NO and ROS synthesis and PGE2 secretion in lipopolysaccharide (LPS)-activated U937 human monocytic cells (derived from a histiocytoma). In order to define the molecular mechanisms underlying the antiproliferative effects of derivative 2, we found that it determined cell cycle arrest at the G1 phase, modified the expression of cell cycle regulatory proteins, and ultimately triggered apoptotic cell death in both breast cancer cell lines. Taken together, these results highlight the studied RSV derivatives, particularly derivative 2, as promising tools for the development of new and more bioavailable derivatives useful in the treatment of breast cancer.  相似文献   
10.
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