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et receptor
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  内皮素受体
     Based on the structure-activity studies of the leading compounds, BQ-123, pentacyclopeptide ETa antagonists and our previous reseach, a new series of cyclopeptide ET receptor antagonists with hydrophobic groups via the L-Lysine amine was designed.
     本课题选择环五肽ET_A受体选择性拮抗剂—BQ-123作为先导化合物,基于文献报道的BQ-123的构效关系研究和课题组前期研究成果,设计了一系列新结构类型的环肽类内皮素受体拮抗剂,并且通过L—赖氨酸的氨基引入疏水基团。
短句来源
     Objective To elucidate whether the distribution of ET-1 and ET receptor (ETR) in local myocardium is different after application of ET_A receptor antagonists during acute myocardial infarction (AMI).
     目的 探讨在急性心肌梗死(AMI)时,使用内皮素受体A拮抗剂(ET_A受体拮抗剂)后对局部心肌组织ET-1和ET受体分布的影响。
短句来源
     Based on the structure-activity studies of the leading compounds, we designed and synthesized a new series of ET receptor antagonists with different N-terminal chemical groups and unnatural amino acids.
     基于先导化合物自身的结构特征,参考文献提供的构效关系研究信息,通过改变N-端结构、引入非天然氨基酸或非氨基酸等方法,设计合成了一系列新结构类型的肽类内皮素受体拮抗剂。
短句来源
     (2) Inhibitory test: The influence of ET 1 inhibitors on the HMC proliferation following thrombin stimulation at three different levels, i.e. ET 1 antiserum, selective ET receptor type A (ET A) antagonist and antisense oligodeoxynucleotide for ppET 1, was measured by MTT test respetively.
     (2)抑制试验:将ET1抗血清、选择性内皮素受体ETA拮抗剂和的反义寡核苷酸分别作为三个不同水平的ET1抑制剂,用MTT方法观察它们对凝血酶诱导的HMC增生的抑制作用。
短句来源
     ET 1(20 nmol/L), with BQ123(a selective antagonist for ET receptor A,1 mmol/L) or with BQ788(a selective antagonist for ET receptor B,1 mmol/L),was added respectively into the cultures simultaneously. And the apoptotic neurons were quantitatively measured with flow cytometry 24 hours later.
     再用流式细胞仪分别定量检测内皮素受体A拮抗剂或内皮素受体B拮抗剂对20nmol/L内皮素1诱导神经元凋亡的效果。
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  “et receptor”译为未确定词的双语例句
     BQ123 (selective antagonist for ET receptor A, 1 mmol/L) and BQ788 (selective antagonist for ET receptor B, 1mmol/L) partially blocked the effect of ET-1 inducing neuron apoptosis (P<0.01), respectively.
     BQ123和BQ788分别部分阻断了20 nmol/L ET-1诱导神经元凋亡的作用(P<0.01),但阻断效果不完全。
短句来源
     NO donor L Arg and ET receptor antagonist TAK 044 could alleviate the hepatic I/R injury in some degree, whereas NO synthase inhibitor L NAME aggravated the damage.
     NO供体L 精氨酸 (L Arg)与ET受体拮抗剂TAK 0 44在一定程度上可减轻肝I/R损伤 ,而NO合酶抑制剂L NAME进一步加重了损伤。
短句来源
     Thereafter, in addition to 10 nM ET-1, BQ123 (a selective ETA receptor antagonist), BQ788 (a selective ETa receptor antagonist) or PD145065 (a non-selective ET receptor antagonist) was simultaneously added into the cultures, respectively, and the medium was collected 6 h after the administration for NO concentration measurement.
     接着,在10 nM ET-1处理的同时,分别加入BQ123(选择性ET_A受体拮抗剂)、BQ788(选择性ET_B受体拮抗剂)、PD145065(非选择性ET受体拮抗剂),作用6h后检测培养基中NO浓度。
短句来源
     Conclusion The higher dose of ET-1 (20 nmol/L) can directly induce apoptosis in primary cultured rat brain neurons, but the lower dose of ET-1. The effect of ET-1 inducing neuronal apoptosis may be mediated via both ET receptor A and B.
     结论20 nmol/L ET-1可直接诱导培养大鼠大脑皮质神经元凋亡,其作用可能是通过其A受体和B受体亚型共同实现的。
短句来源
     BQ123 (selective antagonist for ET receptor A, 1 mM) and BQ788 (selective antagonist for ET receptor B, ImM) partially blocked the effect of ET-1 inducing neuron apoptosis (P<0.01), respectively.
     BQ123和BQ788分别部分阻断了ET-1诱导神经元凋亡的作用(P<0.01),但阻断效果不完全。
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  et receptor
ET receptor density was shown to be significantly higher in the prostate from diabetic rats than those from either control or insulin treated diabetic animals.
      
Thus, the loss of ET receptors as well as the receptor-mediated responses in transformed cells can be explained by down-regulation of ET receptor mRNA.
      
These findings indicate that different subtypes of the ET receptor are responsible for the induction of the positive inotropic effect of ET-3 and ET-1.
      
The nonselective ET receptor antagonist PD 145065 effectively antagonized the positive inotropic effect of ET-3 in a concentration-dependent manner and abolished it at 10-5 M.
      
These results indicate that ET receptor antagonists indeed have a potential to improve hemodynamics, symptoms, and potentially prognosis of CHF which still carries a high mortality.
      
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Endothelin(ET)is a potent vasocontrictor peptide released from vascular endothelial cells.ET also has other biological functions relevant to tumorgenesis,including mitogenic and angiogenic activities. The expression of ET in human bladder cancer tissues and bladder cancer BIU-87 cell line was detected,and the effect of ET on the proliferation of BIU-87 was studied. Northern blot showed that the level of ET-1 mRNA expression was more than 4-fold higher in tumor tissues than the surrounding...

Endothelin(ET)is a potent vasocontrictor peptide released from vascular endothelial cells.ET also has other biological functions relevant to tumorgenesis,including mitogenic and angiogenic activities. The expression of ET in human bladder cancer tissues and bladder cancer BIU-87 cell line was detected,and the effect of ET on the proliferation of BIU-87 was studied. Northern blot showed that the level of ET-1 mRNA expression was more than 4-fold higher in tumor tissues than the surrounding noncancerous tissues (n=4).Using radioimmunoassay,it was also found that the content of ET in tumor tissues was 6-8 fold higher than the surrounding noncancerous tissues (n=4). In BIU-87 cells, the level of ET concentration was increased (38%and 47%) after TPA (100 ng/mL) treatment (4 h and 8 h). The secretion level of ET in BIU-87 cells was also slightly stimulated by TPA (100 ng/mL,8 h). After treated with ET-antiserum,the  ̄3H-TdR incorporation was markedly decreased (57%) in BIU-87 cells whereas it was also decreased (35%) after treated BIU-87 with ET receptor A antagonist──BQ_(123).In conclusion,ET was markedly expressed both in human bladder cancer tissues and BIU-87 cells, especially when the cells were induced by TPA. It seems that ET has proliferative effgct on bladder cancer cells and this effect can be depressed by ET-antiserun or ET receptor A antagonist──BQ_(123).

应用Northernblot杂交技术及放射免疫方法对人膀胱移行细胞癌组织中内皮素-1mRNA及内皮素活性分子的表达水平进行检测,研究了佛波酯对人膀胱移行细胞癌BIU-87细胞中内皮素活性分子表达水平的调节作用,并探讨了内皮素抗血清及内皮素A型受体竞争性拮抗剂BQ_(123)对BIU-87细胞DNA合成的影响。结果表明,人膀胱移行细胞癌组织中内皮素-lmRNA及内皮素活性分子的表达水平明显高于相应的癌旁组织,佛波酯可促进BIU-87细胞合成和分泌内皮素,内皮素抗血清及BQ_(123)可抑制BIU-87细胞合成DNA。提示内皮素在膀胱癌发展及BIU-87细胞恶性增殖中可能起重要作用。

Objective: To investigate the effect of burned serum on the endothelin(ET) receptor in cardiac microvascular endothelial cells(CMEC).Methods: CMEC were isolated and cultured. Following incubation of CMEC with the culture medium containing 20% normal and burned rat(30% TBSA Ⅲ°)serum for 12h, respectively, the affinity and binding capacity of ET receptor in CMEC membranes were measured by radioligand binding assay.Results: Only ETB receptor was distributed in rat CMEC membranes .with a...

Objective: To investigate the effect of burned serum on the endothelin(ET) receptor in cardiac microvascular endothelial cells(CMEC).Methods: CMEC were isolated and cultured. Following incubation of CMEC with the culture medium containing 20% normal and burned rat(30% TBSA Ⅲ°)serum for 12h, respectively, the affinity and binding capacity of ET receptor in CMEC membranes were measured by radioligand binding assay.Results: Only ETB receptor was distributed in rat CMEC membranes .with a maximal binding capacity(Bmax)of 142±27 fmol/mg protein and a dissociation constant(Kd) of 119±22pmol/L.Burned rat serum induced an increase in Bmax of ETB receptor by 68%. without concomitant changes in Kd value. Conclusion: Burned serum may up-regulate ETB receptor.

目的:探讨烧伤血清对心脏微血管内皮细胞内皮素受体的影响。方法:分离和培养大鼠心脏微血管内皮细胞,分别用含20%正常大鼠和烧伤大鼠(30%TBSAⅢ度)伤后6h血清的培养基培养心脏微血管内皮细胞12h,用放射性配基结合分析法,测定内皮细胞膜内皮素受体亲和力及结合容量。结果:大鼠心脏微血管内皮细胞膜上只有亚型B内皮素受体分布,该受体的最大结合容量(Bmax)为142±27fmol/mg,平衡解离常数(Kd)为119±22pmol/L。烧伤血清不影响该受体的Kd值,但使Bmax增加68%。结论:烧伤血清可上调亚型B内皮素受体。

The changes of the quantity and distribution of mRNA of endothelin receptor A (ETA) and endothelin receptor B (ETB) in rat kidneys at different time phases during the early stage after severe burns were dynamically observed. It was found that the percentages of ETA and ETB mRNA in kidneys were significantly elevated at the 1st hour postburn (the former reached its climax on the 3rd while the latter did so on the 6th hour postburn) and ETA mainly expressed in cortex and ETB in medulla. Our findings...

The changes of the quantity and distribution of mRNA of endothelin receptor A (ETA) and endothelin receptor B (ETB) in rat kidneys at different time phases during the early stage after severe burns were dynamically observed. It was found that the percentages of ETA and ETB mRNA in kidneys were significantly elevated at the 1st hour postburn (the former reached its climax on the 3rd while the latter did so on the 6th hour postburn) and ETA mainly expressed in cortex and ETB in medulla. Our findings suggest that the changes of ET receptors participate in damage of the renal function.

动态观察大鼠烧伤早期肾脏各时相点内皮素受体A(ETA)、内皮素受体B(ETB)mRNA定量和分布的变化规律,发现肾脏ETA、ETBmRNA百分占有率在烧伤后1h已明显升高,前者3h达高峰,后者6h达高峰,皮质以ETA为主,髓质以ETB为主,提示烧伤后内皮素受体改变参与了肾功能损害

 
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