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变构调制
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  “变构调制”译为未确定词的双语例句
     Interallosteric modulation of neurotoxins on Na ~+ channel receptor binding sites
     神经毒素对电压门控钠通道受体靶点的变构调制
短句来源
     Conclusion The mechanism of TMP action may be the allosteric regulation via acting on PKA system and the large extracellular region of ATP receptor-ion channel complex(P2X receptors) to affect P2X receptor agonists-activated currents in rat DRG neurons.
     结论川芎嗪可能是通过PKA系统以及P2X受体离子通道复合体细胞外环的变构调制点影响P2X受体激动剂在大鼠DRG神经元的激活电流。
短句来源
     Clarifying the binding properties and interallosteric modulation of neurotoxins on VGSC is valuable not only for enlarging the knowledge of channel proteomics, channel pharmacology and toxicology, but also for designing new channel specific medicine and biologic pesticide.
     全面探明并深刻剖析各种神经毒素与钠通道受体靶点的结合特性以及彼此间的相互变构调制 ,不仅有助于丰富通道蛋白组学、通道药理与毒理学等创新知识 ,也是研制针对性钠通道受体新药和构建环保型生物农药的前提条件。
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  相似匹配句对
     Interallosteric modulation of neurotoxins on Na ~+ channel receptor binding sites
     神经毒素对电压门控钠通道受体靶点的变构调制
短句来源
     (2) The part for modulation signal;
     (2)调制信号源;
短句来源
     Modulation Contrast Microscopy
     调制衬比显微术
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  allosteric modulation
These data are consistent with an allosteric modulation of DHP calcium channel antagonist binding sites by PCP and structural derivatives that is not mediated through the brain PCP binding site.
      
In order to probe the specificity of muscarinic allosteric modulation, we checked whether these agents interact with histamine H1-receptors which have a high homology with muscarinic receptors.
      
Rationale: Neuroactive steroids represent a novel class of potential therapeutic agents (epilepsy, anxiety, migraine, drug dependence) thought to act through positive allosteric modulation of the GABAA receptor.
      
In addition, the effects of pressure on ligand binding were explored to further investigate the mechanism of pressure antagonism of allosteric modulation.
      
The understanding of the molecular mechanism of allosteric modulation of ligand-operated ionic channels by trace metals is a new contribution to metallo-neurobiology.
      
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Voltage gated Na + channel(VGSC)is the target of numerous natural neurotoxins. Clarifying the binding properties and interallosteric modulation of neurotoxins on VGSC is valuable not only for enlarging the knowledge of channel proteomics, channel pharmacology and toxicology, but also for designing new channel specific medicine and biologic pesticide. This short communication will briefly introduce the advance on interallosteric modulation of neurotoxins on Na + channel receptor binding...

Voltage gated Na + channel(VGSC)is the target of numerous natural neurotoxins. Clarifying the binding properties and interallosteric modulation of neurotoxins on VGSC is valuable not only for enlarging the knowledge of channel proteomics, channel pharmacology and toxicology, but also for designing new channel specific medicine and biologic pesticide. This short communication will briefly introduce the advance on interallosteric modulation of neurotoxins on Na + channel receptor binding cites. \[

电压门控钠通道 (VGSC)是许多天然生物神经毒素特异作用的靶受体。全面探明并深刻剖析各种神经毒素与钠通道受体靶点的结合特性以及彼此间的相互变构调制 ,不仅有助于丰富通道蛋白组学、通道药理与毒理学等创新知识 ,也是研制针对性钠通道受体新药和构建环保型生物农药的前提条件。本文侧重各种神经毒素对电压门控钠通道受体靶点的变构调制研究作一简要的进展情况概述。

Aim To explore the modulaory effect of tetramethylpyrazine(TMP) on the responses mediated by P2X receptors.Methods Whole-cell patch-clamp technique was used to study the effects of TMP on P2X receptor agonists-activated currents in freshly isolated rat dorsal root ganglion(DRG) neurons.Results Extracellular application of ATP of 1 to 1000 μmol·L~(-1) activated currents in DRG neurons(n=102).The ATP-activated currents showed rapid desensitization or slow desensitization.Preapplication of TMP(0.1~10 mmol·L~(-1))markedly...

Aim To explore the modulaory effect of tetramethylpyrazine(TMP) on the responses mediated by P2X receptors.Methods Whole-cell patch-clamp technique was used to study the effects of TMP on P2X receptor agonists-activated currents in freshly isolated rat dorsal root ganglion(DRG) neurons.Results Extracellular application of ATP of 1 to 1000 μmol·L~(-1) activated currents in DRG neurons(n=102).The ATP-activated currents showed rapid desensitization or slow desensitization.Preapplication of TMP(0.1~10 mmol·L~(-1))markedly inhibited ATP(100 μmol·L~(1))-activated currents in the majority of the neurons examined(89.2%,91/102).TMP(1 mmol·L~(-1)) reduced α,β-meATP(10 μmol·L~(-1))-activated currents.TMP(1 mmol· L~(-1)) shifted the concentration-response curve of I_(ATP) downward markedly.TMP(1 mmol·L~(-1)) did not alter the reversal potential(0 mV) of ATP-activated currents.TMP(1 mmol·L~(-1)) significantly inhibited ATP(100 μmol·L~(-1))-activated currents potentiated by PGE_2(100 μmol·L~(-1))or SP(0.1 μmol·L~(-1)).Intracellular application of 10 μmol·L~(-1) H89(which is an inhibitor of PKA) reduced the inhibitory effect of TMP on ATP(100 μmol·L~(-1))-activated currents.Conclusion The mechanism of TMP action may be the allosteric regulation via acting on PKA system and the large extracellular region of ATP receptor-ion channel complex(P2X receptors) to affect P2X receptor agonists-activated currents in rat DRG neurons.

目的探讨川芎嗪(tetram ethy1pyrazine,TMP)对嘌呤2X(P2X)受体介导反应的作用。方法在大鼠新鲜分离的背根神经节(dorsal root ganglion,DRG)神经元标本上应用全细胞膜片钳技术记录川芎嗪对P2X受体激动剂激活电流的影响。结果外加ATP(1~1 000μmol.L-1)可引起DRG神经元产生激活电流(n=102),ATP-激活电流(IATP)显示快失敏和慢失敏两种形式的内向电流。预加川芎嗪(0.1~10mmol.L-1)后,大部分(89.2%,91/102)受检细胞可观察到ATP(100μmol.L-1)-激活电流出现明显的抑制作用。川芎嗪(1 mmol.L-1)使α,-βm eATP(10μmol.L-1)-激活电流减小。预加川芎嗪(1 mmol.L-1)后ATP(1~1 000μmol.L-1)激活电流的剂量-效应曲线明显下移。预加川芎嗪(1 mmol.L-1)前后ATP(100μmol.L-1)的I-V曲线反转电位值不变,均接近0 mV。川芎嗪(1 mmol.L-1)可明显抑制被前列腺素E2(100μmol.L-1)或P物质(0.1μmol.L-1)增大的ATP...

目的探讨川芎嗪(tetram ethy1pyrazine,TMP)对嘌呤2X(P2X)受体介导反应的作用。方法在大鼠新鲜分离的背根神经节(dorsal root ganglion,DRG)神经元标本上应用全细胞膜片钳技术记录川芎嗪对P2X受体激动剂激活电流的影响。结果外加ATP(1~1 000μmol.L-1)可引起DRG神经元产生激活电流(n=102),ATP-激活电流(IATP)显示快失敏和慢失敏两种形式的内向电流。预加川芎嗪(0.1~10mmol.L-1)后,大部分(89.2%,91/102)受检细胞可观察到ATP(100μmol.L-1)-激活电流出现明显的抑制作用。川芎嗪(1 mmol.L-1)使α,-βm eATP(10μmol.L-1)-激活电流减小。预加川芎嗪(1 mmol.L-1)后ATP(1~1 000μmol.L-1)激活电流的剂量-效应曲线明显下移。预加川芎嗪(1 mmol.L-1)前后ATP(100μmol.L-1)的I-V曲线反转电位值不变,均接近0 mV。川芎嗪(1 mmol.L-1)可明显抑制被前列腺素E2(100μmol.L-1)或P物质(0.1μmol.L-1)增大的ATP激活电流。通过微电极胞内透析注入PKA抑制剂H89(10μmol.L-1)至胞内,使川芎嗪(1 mmol.L-1)抑制ATP(100μmol.L-1)激活电流的作用减小。结论川芎嗪可能是通过PKA系统以及P2X受体离子通道复合体细胞外环的变构调制点影响P2X受体激动剂在大鼠DRG神经元的激活电流。

 
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