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旋转相关时间
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  rotational correlation time
    The experiments show that before and after combination the conformation of membrane protein, rotational correlation time ( τC) of insulin molecule and the amplitude (h0) of ESR spectra of insulin nitroxide free radical have been obviously changed.
    实验表明胰岛素与其受体结合前后,膜蛋白质的构象、胰岛素分子的旋转相关时间(τ_c)和胰岛素氮氧自由基的ESR波谱振幅(h_0)均发生明显的变化,这些变化均与胰岛素-受体的内噬现象有关系.
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    BUT resulted in obvious oxidative injuries to the structure and functions of membrane proteins: decrement of membrane thiol content, inhibition of the activities of membrane-bound Na~+/K~+-ATPase and Ca~(2+)/Mg~(2+)-ATPase, increase in the W/S ratio and decrease in the rotation correlation time (τ_c) of the membrane proteins.
    BUT对红细胞膜蛋白的结构和功能具有明显的毒性损伤作用,表现为:浓度依赖性地降低细胞膜巯基的含量,抑制细胞膜Na~+/K~+-ATP酶和Ca~(2+)/Mg~(2+)-ATP酶的活性,增加膜蛋白弱固定化与强固定化比率(W/S),明显缩短膜蛋白的旋转相关时间τ_c。
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  rotational correlation time
A share of membrane-bound spin probe was different for chloroplasts and subchloroplast fragments, as well as its rotational correlation time and apparent enthalpy and entropy activation of nitroxide rotational motion.
      
However, the rotational correlation time τ for spin-labeled Bs and its complex with Bn in solution corresponded precisely to their molecular weights.
      
The rotational correlation time of fulleropyrrolineoxyl was found to be about eight times longer than that of 4-oxy-2,2,6,6-tetramethylpiperidine-1-oxyl.
      
The rotational correlation time, τc, of the spin label tempamine has been used for a comparative study of internal microviscosity in normal and in homozygous β-thalassemic erythrocytes.
      
The effective rotational correlation time, σc, of the spin label 5-SASL results about one order of magnitude higher in the presence of 60 mitogen molecules/vesicle.
      
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The insulin nitroxide free radical was first prepared and used to study the kinetic changes of the spectral parameters in the process of combination between the insulit: probe and its receptor. The experiments show that before and after combination the conformation of membrane protein, rotational correlation time ( τC) of insulin molecule and the amplitude (h0) of ESR spectra of insulin nitroxide free radical have been obviously changed. These changes of parameter of ESR spectrum are related to the endocytose...

The insulin nitroxide free radical was first prepared and used to study the kinetic changes of the spectral parameters in the process of combination between the insulit: probe and its receptor. The experiments show that before and after combination the conformation of membrane protein, rotational correlation time ( τC) of insulin molecule and the amplitude (h0) of ESR spectra of insulin nitroxide free radical have been obviously changed. These changes of parameter of ESR spectrum are related to the endocytose of insulin receptor complexes. The combination could rather be inhibited, when the sulfhydryl group, free amino group or hydroxide group of receptor were blocked.

本文首次制备了胰岛素氮氧自由基,研究了胰岛素探针与其受体结合过程中ESR波谱参数的动力学变化.实验表明胰岛素与其受体结合前后,膜蛋白质的构象、胰岛素分子的旋转相关时间(τ_c)和胰岛素氮氧自由基的ESR波谱振幅(h_0)均发生明显的变化,这些变化均与胰岛素-受体的内噬现象有关系.当封闭受体上的巯基、氨基或羟基时,胰岛素与其受体的结合能力便受到一定的阻抑作用.

Aim To study the relationship between cellular membrane fluidity and relative bioavailability ( F r) of protein and peptide drugs combined with absorption enhancers after pulmonary administration in rats. Methods A series of model drug salmon calcitonin (sCT) solutions with 6 absorption enhancers (Brij78, sodium cholate, sodium caprylate, 2-hydroxypropyl-β-cyclodextrin, lecithin and chitosan) were prepared and then delivered to rats by pulmonary route. Serum drug concentration was determined by radioimmunoassay...

Aim To study the relationship between cellular membrane fluidity and relative bioavailability ( F r) of protein and peptide drugs combined with absorption enhancers after pulmonary administration in rats. Methods A series of model drug salmon calcitonin (sCT) solutions with 6 absorption enhancers (Brij78, sodium cholate, sodium caprylate, 2-hydroxypropyl-β-cyclodextrin, lecithin and chitosan) were prepared and then delivered to rats by pulmonary route. Serum drug concentration was determined by radioimmunoassay method. Using the techniques of electron spin resonance and fluorescence polarography, the effects of enhancers on pulmonary cellular membrane fluidity were investigated. Results F r values of sCT solution with some absorption enhancers (Brij78, sodium cholate, sodium caprylate, lecithin and chitosan) were significantly higher than those without enhancers. Brij78, lecithin and sodium caprylate, not only increased membrane lipid fluidity but also loosed the constitution of membrane protein. The effect of sodium cholate on membrane protein was low. Lipid fluidity was reduced and protein constitution was changed markedly, after pulmonary cellular membrane was treated by 0.5% chitosan solution. This result showed that the absorption enhancing of chitosan mainly came from its effects on membrane protein. Corresponded with lower F r after pulmonary administration, 2-hydroxypropyl-β-cyclodextrin (0.5% and 3%) had not significant effects on both lipid fluidity and protein constitution. Conclusion The effects of enhancers on pulmonary absorption of peptide drugs in vivo might be investigated on the grounds of determination of cellular membrane fluidity in vitro .

目的 从肺细胞膜流动性的角度探讨渗透促进剂增加多肽类药物肺部吸收的作用机制。方法 以鲑鱼降钙素 (sCT)为模型药物 ,考查多种渗透促进剂对sCT经肺吸收的促进作用。采用电子自旋共振 (ESR)技术和荧光偏振技术测定旋转相关时间 (τC)及荧光偏振度 (P) ,计算渗透促进剂处理前后膜脂流动性和膜蛋白构象的变化 ,从而考查渗透促进剂增加药物肺部吸收的原因。结果 可以显著促进药物吸收的苄泽 78、卵磷脂、辛酸钠均引起膜脂质流动性的增加 ,同时造成蛋白构象不同程度的松散 ;牛磺胆酸钠对膜蛋白的影响较弱 ;壳聚糖降低膜脂流动性 ,其促渗作用主要来自于改变了膜蛋白的三级结构而使细胞间紧密连接张力减小 ;2 羟丙基 β 环糊精对药物吸收没有明显贡献 ,同时其对膜通透性基本没有影响。结论 考查体外细胞膜流动性的变化为研究渗透促进剂对药物肺部吸收的促进作用提供了重要依据。

 
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