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931.
目的 探究依达拉奉联合瑞舒伐他汀治疗心源性脑梗死的疗效及对血清趋化因子12(CXCL12)、泛素C末端水解酶L1(UCH-L1)、人类软骨糖蛋白-39(HC-gp39)水平的影响。方法 选取2020年3月—2022年4月达州市中心医院收治的90例心源性脑梗死患者作为研究对象,随机分为对照组和观察组,各45例。对照组给予瑞舒伐他汀治疗,观察组给予依达拉奉联合瑞舒伐他汀治疗。比较两组疗效、CXCL12、UCH-L1、HC-gp39、血液流变学指标、血脂水平及美国国立卫生研究院脑卒中量表(NIHSS)评分。结果 观察组总有效率高于对照组(P <0.05)。观察组治疗前后血清CXCL12、UCH-L1、HC-gp39水平的差值高于对照组(P <0.05)。观察组治疗前后全血低切黏度、全血高切黏度及纤维蛋白原水平的差值高于对照组(P <0.05)。观察组治疗前后TC、TG、LDL-C水平的差值高于对照组(P <0.05)。观察组治疗前后NIHSS评分的差值高于对照组(P <0.05)。结论 依达拉奉联合瑞舒伐他汀治疗心源性心肌梗死可有效提高患者临床疗效,改善血液流变学指标、血脂、神经功能及炎症反应。 相似文献
932.
目的 探讨急性脑梗死患者血清补体C1q/肿瘤坏死因子相关蛋白3(CTRP-3)、D-二聚体、可溶性髓样细胞触发受体2(sTREM2)水平及相关临床特征与溶栓后出血性转化(HT)的关系。方法 回顾性分析2018年9月—2022年9月在青海省人民医院接受溶栓治疗的120例急性脑梗死患者的临床资料,根据患者溶栓后是否发生HT分为HT组(30例)、非HT组(90例)。比较两组患者的临床资料及血清CTRP-3、D-二聚体、sTREM2水平。采用多因素逐步Logistic回归分析急性脑梗死患者溶栓后发生HT的危险因素;绘制受试者工作特征(ROC)曲线,分析急性脑梗死患者溶栓后HT预测模型预测HT发生的价值。结果 HT组心房颤动(以下简称房颤)、大面积脑梗死、入院NIHSS评分≥ 15分占比高于非HT组(P <0.05),血清CTRP-3水平低于非HT组(P <0.05),D-二聚体、sTREM2水平高于非HT组(P <0.05)。血清CTRP-3、D-二聚体、sTREM2水平预测急性脑梗死患者溶栓后发生HT的敏感性分别为66.7%(95% CI:0.598,0.756)、70.0%(95% CI:0.607,0.812)、80.0%(95% CI:0.714,0.889),特异性分别为73.3%(95% CI:0.636,0.821)、86.7%(95% CI:0.778,0.923)、86.7%(95% CI:0.747,0.942)。多因素Logistic逐步回归分析结果显示,房颤[O^R=1.237(95% CI:1.103,1.387)]、大面积脑梗死[O^R=2.338(95% CI:1.292,4.231)]、入院NIHSS评分≥ 15分[O^R=2.087(95% CI:1.231,3.538)]、CTRP-3 ≤ 269.265 μg/L [O^R=3.006(95% CI:1.508,5.992)]、D-二聚体≥ 2.625 mg/L [O^R=2.649(95% CI:1.374,5.107)]、sTREM2 ≥ 314.675 ng/L [O^R=2.328(95% CI:1.411,3.841)]是急性脑梗死患者溶栓后发生HT的危险因素(P <0.05)。根据多因素Logistic逐步回归分析结果建立急性脑梗死患者溶栓后HT预测模型,Logit(P) = -33.887 + 0.213×房颤+ 0.849×大面积脑梗死+0.736×入院NIHSS评分+ 1.101×CTRP-3 + 0.974×D-二聚体+ 0.845×sTREM2;ROC曲线分析结果表明,预测模型预测HT发生的敏感性为93.3%(95% CI:0.841,0.991),特异性为87.8%(95% CI:0.808,0.976)。结论 血清CTRP-3、D-二聚体、sTREM2水平与急性脑梗死患者溶栓后HT有关,预测价值较高,且急性脑梗死患者溶栓后HT预测模型预测HT优于各项指标单独预测。 相似文献
933.
目的 探讨血清可溶性髓系细胞触发受体-1(sTREM-1)、降钙素原(PCT)、脑钠肽(BNP)联合检测对老年患者重症肺炎(SP)预后的评估价值。方法 选取2019年2月—2022年1月贵州医科大学附属医院内科重症监护治疗病房(ICU)收治的127例老年SP患者作为研究对象。统计患者入住ICU后28 d的生存情况,并依据是否存活分为生存组和死亡组。对比两组临床资料。多因素Cox回归分析老年SP患者预后的影响因素。制作受试者工作特征(ROC)曲线,以曲线下面积(AUC)评价血清sTREM-1、PCT、BNP及联合检测对老年SP患者预后的评估价值。结果 两组患者性别、年龄、BMI、入住ICU时间、体温、合并基础疾病、吸烟史、饮酒史、机械通气、白细胞计数、白蛋白及血乳酸水平对比,差异无统计学意义(P>0.05)。死亡组病变累及多个肺叶占比和PSI评分、CRP、IL-6、IL-18、sTREM-1、PCT及BNP水平高于生存组(P <0.05)。多因素Cox回归分析结果显示:病变累及多个肺叶[■=2.901(95%CI:1.335,6.305)]、PSI评分[■=2.807(95%... 相似文献
934.
Murasaki Mitsukuni Miura Sadanori 《Progress in neuro-psychopharmacology & biological psychiatry》1992,16(6)
Mitsukuni Murasaki and Sadanori Miura: The Future of 5-HT1A Receptor Agonists. (Aryl-Piperazine Derivatives) Prog. Neuro- Psychopharmacol-& Biol Psychiat, 1992, 16(6): 833–845.
- 1. 1. At present the dominant position among anti-anxiety medications has changed from meprobamate to the benzodiazepine derivatives.
- 2. 2. In order to avoid benzodiazepine's (BZ) undesirable side effects such as impairment of psycho-motor function, memory impairment, low dose dependence and withdrawal symptoms, a third generation anxiolytic agent, buspirone, the focus of the aryl-piperazine group of anti-anxiety agents, has been introduced recently.
- 3. 3. Aryl-piperazine derivatives work as 5-HT1A receptor partial agonists and are known as serotonin normalizers.
- 4. 4. Therefore, they are expected to have not only an anxiolytic function but also an anti-depressant effect as well.
- 5. 5. A characteristic of the aryl-piperazine derivatives is that they have no sedative and muscle relaxant effects, and they do not have BZ's undesirable side-effects, especially in regard to withdrawal symptoms. However they have a rather weak anxiolytic action and a slow onset of action.
- 6. 6. Aryl-piperazine derivatives will not take the place of BZ, but the use of BZ and buspirone as bridge medications, making the most of the strong points of both, can be proposed as a way to compensate for their respective disadvantages.
Keywords: aryl-piperazine derivatives; future of new anxiolytics; 5-HT1A receptor agonist; nonbenzodiazepine anxiolytic 相似文献
935.
Dr. A. Härfstrand K. Fuxe L. Agnati B. Fredholm 《Journal of neural transmission (Vienna, Austria : 1996)》1989,75(2):83-99
Summary Interactions between a 2-adrenoreceptor agonist and neuropeptide Y (NPY) binding sites have been studied in the rat medulla oblongata (MO) using biochemical binding techniques as well as quantitative autoradiography. Tritiated para-amino clonidine (3H-PAC; 2-adrenoceptor agonist), idazoxan (3H-IDA; 2-adrenoceptor antagonist) and iodinated neuropeptide Y (125I-NPY) were used as radioligands. (1) Neuropeptide Y (NPY; 10–8M) but not bovine pancreatic polypeptide (BPP) nor peptide YY (PYY 10nM) increased the KD value of3H-PAC binding sites. However, intraventricular administration of a high dose of NPY (1.25nmol) did not change the3H-PAC binding characteristics in MO membrane preparations of these animals. (2) GTP 10–4 lowered the affinity of3H-PAC binding. NPY (10 nM) had no additional effect, nor did NPYinfluence the GTP induced shift in potency of clonidine to displace3H-IDA from its binding sites. (3) In the autoradiographical experiments NPY (10nM) significantly reduced3H-PAC binding (2nM) in the nucleus tractus solitarius (NTS) area by 35%. (4) When clonidine, either given centrally in vivo (3.75nmol) or in vitro (10 nM) the binding of125I-NPY was reduced (34 and 24%, respectively) in the NTS. When the monoamine receptors were irreversibly blocked in vivo by N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ, 10 g i.e. 24h)125I-NPY (0.5 nM) binding was increased by 137% in the NTS. This effect of EEDQ was prevented by pretreatment with the 2-adrenoreceptor antagonist idazoxan.These results provide support for a direct intramembrane interaction between the 2-receptor and the NPY receptor within the NTS and may be of importance in central cardiovascular regulation. 相似文献
936.
M. H. de Vries F. A. M. Redegeld A. Sj. Koster J. Noordhoek J. G. de Haan R. P. J. Oude Elferink P. L. M. Jansen 《Naunyn-Schmiedeberg's archives of pharmacology》1989,340(5):588-592
Summary Recently, a mutant rat strain was described with a genetic defect for the biliary excretion of organic anions (TR– rats). To determine the possible heterogeneity of the transport systems in liver, intestine and kidney we investigated the transport of the anion 1-naphthol--d-glucuronide (1-NG) in isolated vascularly perfused organ preparations of the rat liver, intestine and kidney of both Wistar rats and TR– rats. 1-NG was administered as such (liver and kidney experiments) or formed intracellularly from 1-naphthol (1-N) (liver and gut experiments). Independent of the type of exposure to 1-NG, the biliary excretion was considerably impaired in TR– rats. In the intestine the total appearance and the vascular/luminal distribution pattern of 1-NG were not significantly different from the values in control rats. Furthermore, no significant disturbance was found with respect to the renal clearance of 1-NG in the TR– rat when compared with the Wistar rat. Thus, the genetic defect in the TR– rat is restricted to an impaired hepatobiliary excretion of 1-NG and does not affect the excretory systems of the intestine and kidney. These results suggest that the excretion of 1-NG by the liver, intestine and kidney involves distinct organ-specific transport systems. 相似文献
937.
M. H. de Vries G. A. Hofman A. Sj. Koster J. Noordhoek 《Naunyn-Schmiedeberg's archives of pharmacology》1989,340(2):239-245
Summary Using the isolated vascularly fluorocarbon emulsion perfused rat small intestine some factors which determine the extent of the intestinal glucuronidation of 1-naphthol to 1-naphthol--d-glucuronide were studied. Increasing the luminal 1-naphthol concentration resulted in a concomitant increase in the 1-naphthol appearance in the vascular perfusate. In contrast, the total appearance of 1-naphthol--d-glucuronide increased less than proportional to the increase in the luminal 1-naphthol concentration. About 88% of the total amount of 1-naphthol--d-glucuronide excreted was released into the vascular perfusate. The capacity-limited intestinal glucuronide efflux is most likely due to saturation of the excretory mechanism for 1-naphthol--d-glucuronide. Decreasing the vascular flow rate influenced both the appearance of 1-naphthol and 1-naphtol--d-glucuronide in the vascular perfusate, whereas the appearance of 1-naphthol--d-glucuronide in the luminal perfusate was essentially flow-independent. A noradrenaline-induced change in the haemodynamic state of the vascular bed (with the total flow kept constant) resulted in a marked decrease in the 1-naphthol vascular concentration. The vascular 1-naphthol--d-glucuronide concentration was only slightly affected. These results indicate that changes in blood flow and blood flow distribution within the intestinal wall can affect the extent of presystemic intestinal metabolism by interfering with the absorption of the parent compound and the efflux of formed conjugates. These parameters can be of paramount importance for causing variable intestinal first-pass effects of drugs in vivo.
Send offprint requests to M. H. de Vries at the above address 相似文献
938.
Y. Hirata K. Fukui Y. Dan H. Matsuoka T. Sugimoto M. Ishii 《European journal of clinical pharmacology》1989,36(6):575-578
Summary The renal and hormonal effects of the 1-adrenoceptor blocker bunazosin were examined in 6 patients with essential hypertension. Oral bunazosin for 4 to 12 weeks significantly decreased mean blood pressure by 10%, increased effective renal blood flow and creatinine clearance by 34% and 37%, respectively, the plasma norepinephrine concentration was elevated by 60%, and the plasma atrial natriuretic peptide level was lowered by 22%. The plasma renin activity and aldosterone concentration were unchanged. Thus, a moderate reduction in blood pressure was produced by bunazosin treatment while maintaining renal perfusion. 相似文献
939.
Testosterone, administered in the form of an inclusion complex with 2-hydroxypropyl--cyclodextrin by subcutaneous injection, enters the circulation in a manner markedly similar to the natural episodic release by the testes. The effects of a regimen of once-a-day administration of complexed testosterone to adult (castrated or intact) rats and to senescent (intact) rats were investigated. Although this procedure left the castrated animals with concentrations of circulatory hormone far below physiological levels for much of the day, a significant improvement in androgen-sensitive behavior and physiology was obtained. Furthermore, the testosterone effects were more pronounced when high doses were used periodically rather than when the same total amount of testosterone was equally divided among doses. The same supplementation to intact rats intensified androgen-sensitive behavior and physiology over normal levels. In senescent rats uniform pulses of the testosterone complex also improved behavior and physiology. Specifically, spermatogenesis was stimulated and, notably, the treatment increased muscle weight without substantial enlargement of the prostate. Since the testosterone–cyclodextrin complex also can be effectively administered as a sublingual tablet, the data suggest that similar regimens may be recommended for elderly men suffering from decreases in muscle mass. 相似文献
940.
Biochemical characterisation of para-aminophenol-induced nephrotoxic lesions in the F344 rat 总被引:5,自引:0,他引:5
Kevin P. R. Gartland Frank W. Bonner John A. Timbrell Jeremy K. Nicholson 《Archives of toxicology》1989,63(2):97-106
The acute biochemical effects of the nephrotoxin p-aminophenol (PAP) were studied in detail using a combination of conventional bioanalytical and 1H-NMR spectroscopic methods. Dosing PAP (25–100 mg/kg) to male F344 rats resulted in a dose-related proximal nephropathy with consequent elevations in urinary enzymes, glucose, and urine total protein as shown by conventional methodology. 1H-NMR spectroscopy at 400 MHz of urine from PAP-treated rats also revealed a characteristic glycosuria, with concomitant amino aciduria. The increased excretion of these compounds indicates functional defects in the proximal tubule and reduced solute reabsorption efficiency. In addition, 1H-NMR urinalysis and conventional enzymatic analysis showed a dose-related lactic aciduria. Other changes detected by 1H-NMR included a dose-related reduction in the excretion of citrate (confirmed by a conventional biochemical method) and an increase in the excretion of acetate. The degree of abnormalities shown by 1H-NMR urinalysis agreed well with histopathological observations and conventional biochemical indices of nephrotoxicity. 1H-NMR urinalysis therefore serves to highlight changes in the excretion of low MW urine components not routinely studied by conventional biochemical analysis.Abbreviations ALP
alkaline phosphatase
- APAP
paracetamol
- BUN
blood urea nitrogen
- GFR
glomerular filtration rate
- GOT
glutamate oxaloacetate transaminase
- LAP
leucine aminopeptidase
- LDH
lactate dehydrogenase
- MW
molecular weight
- NAG
N-acetyl--D-glucosaminidase
- PAP
p-aminophenol
- ppm
parts per million
- TMAO
trimethylamine N-oxide
- UFR
urine flow rate 相似文献