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Xu F Wu H Katritch V Han GW Jacobson KA Gao ZG Cherezov V Stevens RC 《Science (New York, N.Y.)》2011,332(6027):322-327
Activation of G protein-coupled receptors upon agonist binding is a critical step in the signaling cascade for this family of cell surface proteins. We report the crystal structure of the A(2A) adenosine receptor (A(2A)AR) bound to an agonist UK-432097 at 2.7 angstrom resolution. Relative to inactive, antagonist-bound A(2A)AR, the agonist-bound structure displays an outward tilt and rotation of the cytoplasmic half of helix VI, a movement of helix V, and an axial shift of helix III, resembling the changes associated with the active-state opsin structure. Additionally, a seesaw movement of helix VII and a shift of extracellular loop 3 are likely specific to A(2A)AR and its ligand. The results define the molecule UK-432097 as a "conformationally selective agonist" capable of receptor stabilization in a specific active-state configuration. 相似文献
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B. Reynolds P. A. Stevens S. Hughes J. A. Parkinson N. S. Weatherley 《Water, air, and soil pollution》1995,79(1-4):147-170
Hydrochemical data have been collected for between 6 and 9 years from forest harvesting experiments in small catchments (>10 ha) at Plynlimon and Beddgelert, Wales, UK. Felling resulted in rapid increases in NO 3 ? and K+ concentrations at both sites. A maximum of 3.2 mg N L?1 was observed at Plynlimon about one year after the start of felling. Concentrations declined to control stream values (0.5 mg N L?1) after 5 years. At Beddgelert, NO 3 ? concentrations in the manipulated catchments remained above those in the unfelled control catchment for three years, before declining below control values. The NO 3 ? pulse was related to increased rates of mineralization and nitrification in the soil after felling. The initial increase in K+ concentration after felling at Plynlimon was followed by a slow decline, but concentrations were still above those in the control stream after 5 years. From 4 to 8 years after felling at Beddgelert, K+ concentrations fell below and then generally remained lower than control values. The NO 3 ? pulse after felling at Plynlimon sustained inorganic anion concentrations above those in the control stream for the first 18 months after felling. As the NO 3 ? pulse declined, inorganic anion concentrations decreased to below those in the control stream about 4 years after felling. At Beddgelert, the smaller increase in NO 3 ? concentrations had less of an effect on inorganic anion concentrations which decreased after felling relative to values in the control stream. The increase in NO 3 ? was associated with temporary streamwater acidification in the felled catchments due to the increased rates of nitrification and nitrate leaching. At Plynlimon, streamwater filterable Al concentrations declined after felling, but controls on Al behaviour are complex and not explained by simple equilibrium relationships with Al(OH)3 or by variations in inorganic anion concentrations. At Beddgelert, felling had no effect on stream water filterable Al concentrations. Felling at Plynlimon led to a large reduction in streamwater Cl?, Na+ and SO 4 2? concentrations. At Beddgelert reductions in SO 4 2? and ‘sea salt’ ion concentrations were less clear, reflecting the smaller proportions of the catchments which were harvested. Felling had no deleterious effects on water quality, apart from a temporary slight further decline in stream pH at Beddgelert. Increases in NO 3 ? concentrations were short-lived and concentrations were well below drinking water standards. Filterable Al concentrations were already higher than statutory standards, but were not increased or decreased through felling. 相似文献
187.
Insect repellent/antifeedant activity of 2,4-methanoproline and derivatives against a leaf- and seed-feeding pest insect 总被引:1,自引:0,他引:1
Stevens CV Smagghe G Rammeloo T De Kimpe N 《Journal of agricultural and food chemistry》2005,53(6):1945-1948
2,4-methanoproline is a natural product isolated from the seeds of Ateleia herbert smithii Pittier that was formerly suggested to have insect repellent/antifeedant activity; however, this was not tested quantitatively. In this study the insect repellent/antifeedant potency of methanoproline was measured against larvae of the cotton leafworm, Spodoptera littoralis (Boisd.), and adults of the cowpea weevil, Callosobruchus maculatus (F.). In addition, several N-alkyl, amino, and nitrile derivatives of methanoproline with varying stereodemanding substituents were synthesized and also tested. It was shown that in S. littoralis methanoproline itself did not show any significant activity but that derivatives 5, 7, 8, and 10 did show a reasonable repulsive/antifeedant activity that was comparable to the commercial repellent DEET. A significant repellent activity was scored for methanoproline in adults of C. maculatus that was similar to DEET. 相似文献
188.
We review aspects of climate change likely to impact upon the Collembola and mites (microarthropods) of Victoria Land and the Queen Maud Mountains (VLQMM) in the Ross Sea Region of Antarctica. Five important aspects of biological and biological-environmental interactions are identified as key for understanding the impact of climate change on VLQMM microarthropods: (1) Water availability and utilization; (2) mean temperature (which will affect development and population processes) and extreme temperatures (which affect persistence); (3) ultraviolet radiation, although we note that the periods of peak UV irradiance and microarthropod activity do not coincide; (4) dispersal within and between habitats; and (5) potential establishment of invasive species from within and without Antarctica. The current evidence for effects of climate change on VLQMM microarthropods is equivocal, and we advocate targeted experimental and monitoring studies. Finally, we highlight several areas of high priority for future research, particularly on the mite fauna for which detailed information is currently lacking. These are: (1) functional ecology (including thermal biology, feeding and nutrition and water relations); (2) distribution, dispersal and colonization processes and (3) population and community ecology. 相似文献
189.
Tomato spotted wilt virus (TSWV) resistance wasidentified in Y118 (Fla 925-2), an F1BC1S6 tomato line(Lycopersicon esculentum Mill.), derived from a crosswith L. chilense Dun. (LA 1938). This line waspreviously selected for tomato mottle virus (ToMoV)resistance in Florida. Progeny from crosses betweenFla 925-2 and three different TSWV susceptible L.esculentum parents were used in TSWV resistancestudies. A total of 75 F1 and 596 F2 plants from allthree crosses were screened for TSWV resistance. ForF2 plants free of TSWV symptoms, evaluations were madeusing enzyme-linked immunosorbent assay (ELISA). TenF3 populations used for further greenhouse and fieldscreenings were selected from F2 plants found to befree of the virus using visual and ELISA criteria ateach evaluation. One F1 and four F3 lines werestudied under field conditions (Stellenbosch, SouthAfrica) in which 100% of the `Flora-Dade' susceptiblecontrols were severely infected with TSWV. Theresults of the field study clearly establish that TSWVfield resistance is present in the Fla 925-2 (Y118)derived lines. Studies conducted on these linesrevealed that this resistance has the distinctcharacteristic of often `recovering' from initiallyhigh levels of virus titer in the tissue to levelsbelow detection with ELISA. 相似文献
190.
de la Sancha Noé U. Boyle Sarah A. McIntyre Nancy E. Brooks Daniel M. Yanosky Alberto Cuellar Soto Ericka Mereles Fatima Camino Micaela Stevens Richard D. 《Landscape Ecology》2021,36(10):2997-3012
Landscape Ecology - The Dry Chaco spans more than 87 million hectares across Argentina, Bolivia, and Paraguay. This unique forest system has experienced extensive loss and fragmentation due to... 相似文献