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51.
Dr. Aimee J. Marko Mykhaylo Dukh Dr. Nayan J. Patel Joseph R. Missert Prof. Dr. Tymish Ohulchanskyy Walter A. Tabaczynski Dr. Kei Ohkubo Prof. Dr. Shunichi Fukuzumi Prof. Dr. Rutao Yao Prof. Dr. Munawwar Sajjad Prof. Dr. Ravindra K. Pandey 《ChemMedChem》2019,14(16):1503-1513
Herein we report the synthesis, photophysical properties, positron emission tomography (PET) imaging and photodynamic therapy (PDT) efficacy of methyl 3-(1′-m-iodobenzyloxy)ethyl-3-devinyl-verdin 4 (with or without the 124I isotope). The PET imaging ability and ex vivo biodistribution of [124I] 4 were compared with the well-studied methyl [3-(1241′-m-iodobenzyloxy)ethyl]-3-devinyl-pyropheophorbide-a methyl ester (PET-ONCO or [124I] 2 ) and [18F]fluorodeoxyglucose ([18F]FDG) in BALB/c mice bearing colon-26 tumors. Whole-body PET images of [124I] 4 containing a fused methoxy cyclohexenone ring system showed excellent tumor contrast with time (72>48>24 h post-injection). Ex vivo biodistribution results indicate that relative to the current clinical standard [18F]FDG and [124I] 2 in 2 % ethanol formulation, [124I] 4 , at the same radioactive dose (25 μCi per mouse), showed higher tumor uptake at 24 h post-injection and longer tumor retention. In biological environments, compound 4 showed lower fluorescence and lower singlet oxygen yield than 2 , which is possibly due to higher aggregation caused by the presence of a fused cyclohexenone ring system, resulting in limited in vitro/in vivo PDT efficacy. Therefore, the chlorophyll-a analogue [124I] 4 provides easy access to a novel PET imaging agent (with no skin phototoxicity) to image cancer types—brain, renal carcinomas, pancreas—in which [18F]FDG shows limitations. 相似文献
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53.
Dr. Xiaoyun Deng Dr. Akiko Hatori Dr. Zhen Chen Dr. Katsushi Kumata Dr. Tuo Shao Dr. Xiaofei Zhang Dr. Tomoteru Yamasaki Dr. Kuan Hu Dr. Qingzhen Yu Dr. Longle Ma Dr. Gangqiang Wang Dr. Lu Wang Prof. Dr. Yihan Shao Prof. Dr. Lee Josephson Prof. Dr. Shaofa Sun Prof. Dr. Ming-Rong Zhang Prof. Dr. Steven Liang 《ChemMedChem》2019,14(3):303-309
Muscarinic acetylcholine receptors (mAChRs) have five distinct subunits (M1–M5) and are involved in the action of the neurotransmitter acetylcholine in the central and peripheral nervous system. Attributed to the promising clinical efficacy of xanomeline, an M1/M4-preferring agonist, in patients of schizophrenia and Alzheimer's disease, M1- or M4-selective mAChR modulators have been developed that target the topographically distinct allosteric sites. Herein we report the synthesis and preliminary evaluation of 11C-labeled positron emission tomography (PET) ligands based on a validated M4R positive allosteric modulator VU0467485 (AZ13713945) to facilitate drug discovery. [11C]VU0467485 and two other ligands were prepared in high radiochemical yields (>30 %, decay-corrected) with high radiochemical purity (>99 %) and high molar activity (>74 GBq μmol−1). In vitro autoradiography studies indicated that these three ligands possess moderate-to-high in vitro specific binding to M4R. Nevertheless, further physiochemical property optimization is necessary to overcome the challenges associated with limited brain permeability. 相似文献
54.
Sevim Demirozu Senol 《International Journal of Applied Ceramic Technology》2019,16(1):138-145
This study investigates the effect of Li and Mg codoping on the structural, optical, and electrical properties of the ZnO. Zn0.95−xLi0.05MgxO (x = 0.00, 0.01, 0.02, 0.03) nanoparticles are synthesized by hydrothermal method. X-ray diffraction (XRD) results confirmed that all samples are polycrystalline with a hexagonal-wurtzite structure. The surface morphology of the samples were examined by Scanning Electron Microscopy (SEM). The SEM analysis showed that all samples exhibit cheese-like plates and the plate sizes increase with Mg addition. Optical properties were examined by UV-VIS diffuse reflectance spectroscopy. The optical measurements indicate that the reflectance edge of the samples have red shift up to 2% Mg doping level, but blue-shift for 3% Mg doping. The optical band gap of Zn0.95−xLi0.05MgxO nanostructures are calculated as 3.227, 3.214, 3.209, and 3.221 eV with x = 0.00, 0.01, 0.02, 0.03 respectively. Electrical properties including the carrier concentration, Hall mobility, and resistivity were studied using Van-der Pauw method. The temperature resistivity curves of the samples shown typical semiconductor behavior. The carrier concentration decreases with increasing doping level up to 2% Mg, and it slightly increases for 3% Mg. The variation of the Hall mobility for the samples is inversely proportional to the carrier concentration. 相似文献
55.
Abdullah Ameen Saad Hassan Wasi Khan Shahid Husain Pooja Dhiman Mahavir Singh 《International Journal of Applied Ceramic Technology》2020,17(5):2430-2438
In this work, the physical properties of nanocrystalline samples of La0.7Sr0.3Mn1−xFexO3 (0.0 ≤ x ≤ 0.20) perovskite manganites synthesized by the reverse micelle (RM) technique were explored in detail. The phase purity, crystal structure, and crystallite size of the samples were determined using X-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy. All the samples had rhombohedral crystal structure and crystallite size increased with increase in Fe content in La0.7Sr0.3MnO3. The scanning electron micrographs (SEMs) exhibited smooth surface morphology and nonuniform shape of the particles. The optical properties studied using UV-visible absorption spectroscopy revealed a decrease in the absorbance and optical band gap with an increase in Fe content in La0.7Sr0.3MnO3 compound. The temperature-dependent resistivity measurements revealed semiconducting nature of x = 0 and 0.1 samples up to the studied temperature range, while a metal-to-insulator transition was observed at higher Fe doping. Magnetic studies revealed weak ferromagnetism in all the samples and a reduction in the maximum magnetization with an increase in Fe content. A close correlation between electrical transport and magnetic properties was observed with the doping of Fe ion in La0.7Sr0.3MnO3 at Mn site. These results advocate strong interactions associated with the double exchange mechanism among Fe3+ and Mn3+ ions. 相似文献
56.
C. BOULOGNE C. GILLET L. HUGHES R. LE BARS A. CANETTE C.R. HAWES B. SATIAT-JEUNEMAITRE 《Journal of microscopy》2020,280(2):86-103
Up-to-date imaging approaches were used to address the spatiotemporal organisation of the endomembrane system in secretory cells of Dionaea muscipula. Different ‘slice and view’ methodologies were performed on resin-embedded samples to finally achieve a 3D reconstruction of the cell architecture, using ultrastructural tomography, array tomography, serial block face-scanning electron microscopy (SBF-SEM), correlation, and volume rendering at the light microscopy level. Observations of cryo-fixed samples by high-pressure freezing revealed changes of the endomembrane system that occur after trap activation and prey digestion. They provide evidence for an original strategy that adapts the secretory machinery to a specific and unique case of stimulated exocytosis in plant cells. A first secretion peak is part of a rapid response to deliver digestive fluids to the cell surface, which delivers the needed stock of digestive materials ‘on site’. The second peak of activity could then be associated with the reconstruction of the Golgi apparatus (GA), endoplasmic reticulum (ER) and vacuolar machinery, in order to prepare for a subsequent round of prey capture. Tubular continuum between ER and Golgi stacks observed on ZIO-impregnated tissues may correspond to an efficient transfer mechanism for lipids and/or proteins, especially for use in rapidly resetting the molecular GA machinery. The occurrence of one vacuolar continuum may permit continuous adjustment of cell homeostasy. The subcellular features of the secretory cells of Dionaea muscipula outline key innovations in the organisation of plant cell compartmentalisation that are used to cope with specific cell needs such as the full use of the GA as a protein factory, and the ability to create protein reservoirs in the periplasmic space. Shape-derived forces of the pleiomorphic vacuole may act as signals to accompany the sorting and entering flows of the cell. 相似文献
57.
针对日益严峻的食品安全问题,特别是食源性致病菌的快速检测,本文提出一种基于表面改性石墨烯粗锥型马赫-曾德尔干涉结构的光纤大肠杆菌传感器。首先,截取一根4 cm的实心光子晶体光纤,两端分别与两根单模光纤进行粗锥熔接,形成基于马赫-曾德尔干涉原理的传感结构;接着,制备一种表面改性石墨烯敏感材料,将它涂覆在实心光子晶体光纤的表面,使传感器对大肠杆菌溶液有较高的灵敏度;最后,将上述传感器置于水槽中,以此检测大肠杆菌溶液浓度。实验结果表明,在大肠杆菌溶液浓度为50~600 cfu/mL内,随着菌液的浓度增大,传感器的干涉光谱发生了明显的蓝移,灵敏度为3.43 pm/(cfu·mL^-1),菌液浓度与波长偏移的线性度为0.95649,检测限为67.18 cfu/mL,响应时间为15 s。该传感器成本低、体积小、响应时间快,适用于低浓度大肠杆菌浓度的快速检测。 相似文献
58.
为了研究反压压力对成型厚壁光学透镜的影响,利用自行开发的分层反压注射成型厚壁光学透镜的实验方案,通过正交实验优化设计开展了工艺参数优化实验,研究了在不同分层方式下内外层反压压力对对厚壁光学透镜光学性能的影响,从而根据正交优化参数组合成型具有优异光学性能的理想厚壁光学透镜。 正交实验研究结果表明,使用聚甲基丙烯酸甲酯(PMMA)为厚壁光学透镜的原材料进行分层反压注射成型,能够有效减少厚壁光学透镜收缩率,同时随着内外层反压压力的提高,厚壁光学透镜的透光率和折射率均不同程度的得到提高,透镜光学性能优异。 相似文献
59.
高折射率和非线性光学玻璃可以用于高速光开关、光学存储器、新型光纤和光学运算元件等,其研究受到各国科技工作者的高度重视,本文采用熔融淬冷法制备了组成为(85-x)B2O3-15K2O-xSb2O3(x=70, 75, 80, 85)的4组玻璃,测试了玻璃样品的密度、折射率、热学性能、拉曼光谱和吸收光谱,利用玻璃样品的吸收光谱计算了其直接允许光学带隙、间接允许光学带隙及Urbach能量。结果表明:随着Sb2O3含量的增加,玻璃样品的密度从4.445g/cm3逐渐增加到4.767g/cm3,折射率从1.9438增加到2.0058,玻璃转变温度从291℃降低到260℃,玻璃析晶温度从463℃降低到370℃,直接光学带隙从3.2775eV降低到3.1379eV,间接光学带隙从3.1444eV降低到3.0256eV,Urbach能量从0.137eV逐渐减小到0.107eV。说明Sb2O3-K2O-B2O3系统玻璃可以作为新型的非线性光学玻璃候选材料之一。 相似文献
60.
随着自主式水下机器人的发展,水下探测技术成为新的研究热点。然而,吸收效应和散射效应导致水下获取的图像存在雾化和色彩偏差等缺陷。降质的水下图像在一定程度上降低了水下目标识别的准确性。为了改善水下图像质量,国内外学者对水下图像处理方法进行了深入研究。因水下图像处理方法对提升水下目标识别准确性具有良好的促进作用,故其具有重要的研究与分析价值。介绍了水下成像模型,分析了水下图像视觉质量下降的原理;根据水下物理成像模型将水下图像处理方法分为水下图像增强与水下图像复原,并分别对两类方法的研究现状进行分析与归纳;最后,总结与讨论了各类方法的优缺点,并展望了未来的发展方向。 相似文献