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81.
A rapid and sensitive fluorescence-based bioassay for determination of indoleamine 2,3-dioxygenase (IDO) activity has been developed. This assay relies on the quantification of the amount of kynurenine produced in the assay medium by fluorescence and complements the standard absorbance and high-performance liquid chromatography (HPLC) assay methods. The fluorescence method has limits of detection similar to those of the standard assay methods. Measured activities of IDO, including in the presence of tryptophan-based inhibitors, were in statistical agreement with the absorbance and HPLC assay methods. The fluorescence-based assay was also suitable for assessment of IDO inhibition by compounds that are incompatible with the absorbance method. 相似文献
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The association of the sulphogalactosylglycerolipid of rat brain with myelination 总被引:1,自引:1,他引:1 下载免费PDF全文
Joanne Pieringer G. Subba Rao Paul Mandel Ronald A. Pieringer 《The Biochemical journal》1977,166(3):421-428
The sulphogalactosylglycerolipid of rat brain is closely associated with the process of myelination, as demonstrated by the following observations. 1. The lipid is barely detectable in rat brain before 10 days of age, accumulates rapidly between age 10 and 25 days, and remains relatively constant in amount (between 0.3 and 0.4mumol per brain) thereafter into adult life. 2. The activity of adenosine 3'-phosphate 5'-sulphatophosphate-galactosyldiacylglycerol sulphotransferase is almost absent before 10 days of age, attains a maximum at age 20 days, and slowly decreases thereafter with increasing age. This developmental pattern correlates well with that of other myelin-specific metabolites. 3. Both the concentration of the sulphogalactosylglycerolipid and the activity of sulphotransferase are greatly decreased in the non-myelinating jimpy mouse. 4. The myelin fraction of rat brain contains most of the sulphogalactosylglycerolipid. The lipid occurs in a diacyl and an alkylacyl form. Determinations of the relative amount of each type in brain showed about a 1:1 mixture in both 21-day-old and adult rats. Rats injected with H(2) (35)SO(4) at 20 days of age lost (35)S from the diacyl form at a higher rate than from the alkylacyl compound over a 21-day period. These data suggest that the diacyl form has a higher turnover than the alkylacyl derivative. The percentage of the total sulpholipid content of brain contributed by the sulphogalactosylglycerolipid is 16% in 21-day-old rats and 8.4% in adult rats. 相似文献
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Yolima Carrillo Elise Pendall Feike A. Dijkstra Jack A. Morgan Joanne M. Newcomb 《Plant and Soil》2011,347(1-2):339-350
Warming and elevated atmospheric CO2 (eCO2) can elicit contrasting responses on different SOM pools, thus to understand the effects of combined factors it is necessary to evaluate individual pools. Over two years, we assessed responses to eCO2 and warming of SOM pools, their susceptibility to decomposition, and whether these responses were mediated by plant inputs in a semi-arid grassland at the PHACE (Prairie Heating and CO2 Enrichment) experiment. We used long-term soil incubations and assessed relationships between plant inputs and the responses of the labile and resistant pools. We found strong and contrasting effects of eCO2 and warming on the labile C pool. In 2008 labile C was increased by eCO2 and was positively related to plant biomass. In contrast, in 2007 eCO2 and warming had interactive effects on the labile C, and the pool size was not related to plant biomass. Effects of warming and eCO2 in this year were consistent withtreatment effects on soil moisture and temperature and their effects on labile C decomposition. The decomposition rate of the resistant C was positively related to indicators of plant C inputs. Our approach demonstrated that SOM pools in this grassland can have early and contrasting responses to climate change factors. The labile C pool in the mixed-grass prairie was highly responsive to eCO2 and warming but the factors behind such responses were highly dynamic across years. Results suggest that in this grassland the resistant C pool could be negatively affected by increases in plant-production driven available soil C. 相似文献
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David M. Wilson James Apps Nicholas Bailey Mark J. Bamford Isabel J. Beresford Michael A. Briggs Andrew R. Calver Barry Crook Robert P. Davis Susannah Davis David K. Dean Leanne Harris Tom D. Heightman Terry Panchal Christopher A. Parr Nigel Quashie Jon G.A. Steadman Joanne Schogger Andrew D. Medhurst 《Bioorganic & medicinal chemistry letters》2013,23(24):6897-6901
This Letter describes the discovery of a novel series of H3 receptor antagonists. The initial medicinal chemistry strategy focused on deconstructing and simplifying an early screening hit which rapidly led to the discovery of a novel series of H3 receptor antagonists based on the benzazepine core. Employing an H3 driven pharmacodynamic model, the series was then further optimised through to a lead compound that showed robust in vivo functional activity and possessed overall excellent developability properties. 相似文献
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The inhibitory activity of natural products on plant p-hydroxyphenylpyruvate dioxygenase 总被引:3,自引:0,他引:3
Meazza G Scheffler BE Tellez MR Rimando AM Romagni JG Duke SO Nanayakkara D Khan IA Abourashed EA Dayan FE 《Phytochemistry》2002,60(3):281-288
The inhibitory activity of 34 natural products of various structural classes on hydroxyphenylpyruvate dioxygenase (HPPD), the target site for triketone herbicides, and the mode of interaction of selected natural products were investigated. Recombinant HPPD from arabidopsis is sensitive to several classes of natural compounds including, in decreasing order of sensitivity, triketones, benzoquinones, naphthoquinones and anthraquinones. The triketone natural products acted as competitive tight-binding inhibitors, whereas the benzoquinones and naphthoquinones did not appear to bind tightly to HPPD. While these natural products may not have optimal structural features required for in vivo herbicidal activity, the differences in their kinetic behavior suggest that novel classes of HPPD inhibitors may be developed based on their structural backbones. 相似文献
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Verena Liedschulte Hélène Laparra James Nicolas Duncan Battey Joanne Deborah Schwaar Hervé Broye Régis Mark Markus Klein Simon Goepfert Lucien Bovet 《Plant, cell & environment》2017,40(3):364-377
In tobacco, the heavy metal P1B‐ATPases HMA4.1 and HMA4.2 function in root‐to‐shoot zinc and cadmium transport. We present greenhouse and field data that dissect the possibilities to impact the two homeologous genes in order to define the best strategy for leaf cadmium reduction. In a first step, both genes were silenced using an RNAi approach leading to >90% reduction of leaf cadmium content. To modulate HMA4 function more precisely, mutant HMA4.1 and HMA4.2 alleles of a Targeting Induced Local Lesions IN Genomes (TILLING) population were combined. As observed with RNAi plants, knockout of both homeologs decreased cadmium root‐to‐shoot transfer by >90%. Analysis of plants with segregating null and wild‐type alleles of both homeologs showed that one functional HMA4 allele is sufficient to maintain wild‐type cadmium levels. Plant development was affected in HMA4 RNAi and double knockout plants that included retarded growth, necrotic lesions, altered leaf morphology and increased water content. The combination of complete functional loss (nonsense mutation) in one homeologous HMA4 gene and the functional reduction in the other HMA4 gene (missense mutation) is proposed as strategy to limit cadmium leaf accumulation without developmental effects. 相似文献