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1.
The drug‐transporting proteins can affect the pharmacokinetics and pharmacodymanics of many drugs, resulting in an erratic and unpredictable pharmacological response. The Caco‐2 monolayer is routinely applied to investigate the carrier‐mediated transport of drugs. Therefore, the selection of a marker compound able to characterize the activity of such transporters is crucial. Fexofenadine (FEX), a P‐gp/OATP substrate, can be considered a suitable probe. However, in order to use be used as a marker compound, it is mandatory to develop an analytical method able to quantify this drug during the in vitro permeability assay. An HPLC method with ultraviolet detection was developed; the mobile phase consisted of phosphate buffer (pH 3.2) containing 10 m m of sodium octanosulphonate and acetonitrile (60:40) and the flow rate was set at 1.2 mL/min. Fexofenadine was eluted at 40°C, the retention time was about 4.6 min. The LOD and LOQ values were 1.9 and 6.2 ng/mL, respectively. Verapamil and ketoconazole, the most common P‐gp inhibitors, were eluted as distinct peaks of that corresponding to fexofenadine The method was successfully applied to quantify the amount of FEX transported across the Caco‐2 monolayer and could be an additional tool for those investigating the role of membrane transporters on drug absorption. Copyright © 2014 John Wiley & Sons, Ltd.  相似文献   
2.
Recently, oral absorption of cyclic hexapeptides was improved by N‐methylation of their backbone amides. However, the number and position of N‐methylations or of solvent exposed NHs did not correlate to intestinal permeability, measured in a Caco‐2 model. In this study, we investigate enantiomeric pairs of three polar and two lipophilic peptides to demonstrate the participation of carrier‐mediated transporters. As expected, all the enantiomeric peptides exhibited identical lipophilicity (logD7.4) and passive transcellular permeability determined by the parallel artificial membrane permeability assay (PAMPA). However, the enantiomeric polar peptides exhibited different Caco‐2 permeability (Papp) in both directions a–b and b–a. The same trend was observed for one of the lipophilic peptide, whereas the second lipophilic enantiomer pair showed identical Caco‐2 permeability (within the errors). These findings provide the first evidence for the involvement of carrier‐mediated transport for peptides, especially for those of polar nature.  相似文献   
3.
A nonlinear model for a steady flow in a deformable porous medium is considered. The flow is governed by the poroelasticity system consisting of an elasticity equation for the displacement of the porous medium and Darcy's equation for the pressure in the fluid. This poroelasticity system is nonlinear when the permeability in Darcy's equation is assumed to depend on the dilatation of the porous medium. Existence and uniqueness of a weak solution of this poroelasticity system is established under rather weak assumptions on the regularity of the data. Convergence of a finite element approximation is proved and verified through numerical experiments. Copyright © 2013 John Wiley & Sons, Ltd.  相似文献   
4.
As a kind of ammonia‐oxidizing bacteria, Nitrosomonas europaea (N. europaea) was chosen as a research model to study the alteration of cell membrane in the presence of tourmaline and biodegradation of acetochlor. atomic force microscopy images reveal that the presence of tourmaline substantially changes the structure of the outer membrane of the cell responsible for the cell permeability. SEM images show that the introduction of tourmaline makes the cell lose its ability to resist lysozyme owing to the damages. The fluorescence polarization has shown a significant decrease in membrane fluidity and the increase of permeability of cell membrane. Ca2+ and Mg2+ was measured using inductively coupled plasma mass spectrometry and was found in the supernatant from the cells treated by tourmaline. Tourmaline can improve the efficiency of biodegradation of acetochlor for N. europaea. It is proposed that the cell permeability is slightly increased, and the absorbability of nutrition from the medium becomes easier. As a result, N. europaea grows faster in the presence of tourmaline than the native cells. Copyright © 2014 John Wiley & Sons, Ltd.  相似文献   
5.
A series of meso‐ester‐substituted BODIPY derivatives 1–6 are synthesized and characterized. In particular, dyes functionalized with oligo(ethylene glycol) ether styryl or naphthalene vinylene groups at the α positions of the BODIPY core ( 3 – 6 ) become partially soluble in water, and their absorptions and emissions are located in the far‐red or near‐infrared region. Three synthetic approaches are attempted to access the meso‐carboxylic acid (COOH)‐substituted BODIPYs 7 and 8 from the meso‐ester‐substituted BODIPYs. Two feasible synthetic routes are developed successfully, including one short route with only three steps. The meso‐COOH‐substituted BODIPY 7 is completely soluble in pure water, and its fluorescence maximum reaches around 650 nm with a fluorescence quantum yield of up to 15 %. Time‐dependent density functional theory calculations are conducted to understand the structure–optical properties relationship, and it is revealed that the Stokes shift is dependent mainly on the geometric change from the ground state to the first excited singlet state. Furthermore, cell staining tests demonstrate that the meso‐ester‐substituted BODIPYs ( 1 and 3 – 6 ) and one of the meso‐COOH‐substituted BODIPYs ( 8 ) are very membrane‐permeable. These features make these meso‐ester‐ and meso‐COOH‐substituted BODIPY dyes attractive for bioimaging and biolabeling applications in living cells.  相似文献   
6.
Enhanced permeation and retention(EPR) targeting effect of rhodamine B labeled PEG-b-P(LA-co-DHP) [PEG:poly(ethylene glycol);LA:L-lactide;DHP:2,2-dihydroxylmethyl-propylene carbonate] micelles(RhB-micelles) was observed in H22 liver cancer bearing mice.The RhB-micelles were prepared by conjugating rhodamine B with the DHP units of amphiphilic block copolymer PEG-b-P(LA-co-DHP) followed by subsequent self-assembling of the conjugate.The parent copolymer PEG-b-P(LA-co-DHP) was synthesized by ring-opening copo...  相似文献   
7.
郭云胜 《大学物理》2011,(9):24-25,37
以左手材料中产生负磁导率的开口谐振环结构模型为例,从磁导率的定义出发,借助于电磁感应定律,推导了负磁导率的产生过程.  相似文献   
8.
9.
应用NiZn铁氧体的宽带传输线变压器性能分析   总被引:3,自引:0,他引:3       下载免费PDF全文
研究了变换比为4∶1的宽频带传输线变压器,给出了考虑线圈互耦的等效电路模型,分析了其阻抗变换特性。针对在以往传输线变压器分析中忽略频率变化对磁导率的影响这一问题,以应用NiZn铁氧体的宽带传输线变压器为例,将频率变化对磁导率的影响应用到分析传输线变压器特性中。对测试结果的分析和比较表明:在传输线变压器输入阻抗的分析中,频率对其的影响是存在的,在等效电路模型分析中加以考虑,可以更好地与实际值吻合。  相似文献   
10.
感应脉冲加速器的磁芯通常为铁氧体或非晶材料,而感应腔磁芯在工作脉冲下的磁性能是决定感应加速脉冲波形好坏的重要因素。搭建了低压多脉冲实验平台对铁氧体和非晶小磁环分别进行MHz重复频率的多脉冲励磁,对励磁线圈上的电压电流波形进行监测,绘制了多脉冲励磁下磁环的磁化曲线,并结合含磁芯线圈动态电感量的递推公式计算出磁环在多脉冲励磁过程中磁导率的变化曲线;在高压三脉冲实验平台上对铁氧体磁芯和非晶磁芯实验感应腔进行了高压三脉冲实验,得到的磁芯多脉冲磁化规律与低压实验的结果一致。最后对两种磁环在多脉冲励磁下的磁性能差异进行了对比分析。  相似文献   
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