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In clinical. acetylcholinesterase inhibitors reduce the breakdown of synaptic acetylcholine, have been modestly effective in improving the cognitive deficits of Alzheimer's disease.The goal of this work is to determine enzyme kinetics and mechanisms of acetylcholinesterase and butyrlcholinesterase inhibition by five cardiovascular drugs, lovastatin, simvastatin, amlodipine besylate, nifedipine, and hydralazine hydrochloride, and two benzodiazepines, diazepam and chlordiazepoxide hydrochloride. All drugs in this study are reversible mixed-type inhibitors of acetylcholinesterase and butyrylcholinesterase. The pKi values for acetylcholinesterase and butyrylcholinesterase inhibition by the cardiovascular drugs are linearly correlated with the molecular weights of the drugs with the slopes of 0.005 and 0.0021, respectively. Therefore, van der Waals' interactions between acetylcholinesterase and the cardiovascular drugs are stronger than those between butyrylcholinesterase and the drugs. This is probably due to a smaller active site gorge and a more significant peripheral anionic substrate binding site of acetylcholinesterase than those of butyrylcholinesterase.

本研究之目的系决定乙醯胆碱酯酵素和丁醯胆碱酯酵素被五种心脏血管药物lovastatin, simvastatin, amlodipine besylate, nifedipine、hydralazine hydrochloride和两种benzodiazepines:diazepam和Chlordiazepoxide hydrochloride的抑制作用之动力学及机转,这些药物都是乙醯胆碱酯酵素和丁醯胆碱酯酵素的可逆性、混合型之抑制剂,实验结果显示,五种心血管药物对於乙醯胆碱酯酵素及丁醯胆碱酯酵素抑制之pKi值和药物之分子量呈直线之关系,斜率分别为0.005及0.0021因此丁醯胆碱酯酵素,与心血管药物间之凡德瓦作用(van der Waals' )比乙醯胆碱酯酵素与心血管药物间者弱,这可能原因是丁醯胆碱酯酵素之活性区域比乙醯胆碱酯酵素之活性区域更宽广,但丁醯胆碱酯酵素之周边阴离子区域不及乙醯胆碱酯酵素之周边阴离子区域者明显重要,由於五种心血管药物对於乙醯胆碱酯酵素和丁醯胆碱酯酵素抑制之pKi值存在著线性关系表示此种抑制作用系经过共同之反应机理。

The results indicate that female wasps deposit HMPs on the chorion of host eggs with her ovipositor near the end of egg-laying process. Na ye females do not posses the ability for recognizing the marking pheromones and have to obtain the ability though the learning process, in which the wasp inserts her ovipositor into a host egg to determine whether the egg has been parasitized followed by antennal drumming on the exterior. Once the learning process is completed, the female wasp will be able to discriminate between parasitized and unparasitized hosts and reject a parasitized egg by simply drumming on the exterior of the egg. Learning plays an important role in reducing initial rejection time when an unsuitable host is encountered. Female wasps of T. astriniae can quickly learn to associate the presence of a HMP on host egg chrion with the internal status of the egg.

研究结果表明,玉米螟赤眼蜂的寄主标记信息素是在其产卵过程中的收场阶段由产卵器产生的,并且标记在寄主卵表的化学物质;玉米螟赤眼蜂对标记信息素的识别不具有先天性,其必须先用产卵器插入寄生卵来检测是否被寄生,然后其触角不停地敲击,通过学习获得对标记信息素的识别能力,从而放弃了对寄生卵的选择,学习对初始放弃时间有着重要影响,改善了其对寄主搜索效率,这种学习行为是与寄主联系在一起学习的,它能根据寄主被寄生与否而对标记信息素作出反应与不反应。

Aside from pancreatic enzymes activiation and autodigestive process, recent investigations have established that the upregulation of inflammatory mediator are believed to be the critical steps in the progression of mild pancreatitis to severe pancreatitis. Tumor necrosis factor-, ThyomboxaneA2 ,ProstaglandinsI2 are all important inflammatory mediator. TNF-( is one of cytokines. It is important to the over-production of ICAM-1,VCAM-1, TXA2 andPGI2. The ICAM-1 and VCAM-1 mediate both leukocytes adhesion and migration through the endothelium into tissues to connect with injuried target cells. The TXA2 and PGI2 are the production of arachidonic acid. They are responsible for the tissue ischaemia.

肿瘤坏死因子(Tumor necrosis factor-, TNF-、血栓素A2(ThyomboxaneA2,TXA2),前列环素(ProstaglandinsI2,PGI2)均是炎症反应中重要的炎性介质,其中肿瘤坏死因子-是非常重要的细胞因子之一,它由活化的单核细胞产生,在细胞间黏附分子(Intercellular adhesion molecule-1,ICAM-1)及血管细胞黏附分子(Vascular cell adhesion molecule-1,VCAM-1的表达、血栓素A2及前列环素过量生成方面起着重要的作用,前两者是介导白细胞与内皮细胞黏附,迁移于组织并与受损的靶细胞相结合的主要媒介,是炎症反应中的重要介质,后两者是花生四烯酸的代谢产物,亦是重要的炎性介质,参与构成血液循环障碍。

Similarly, IVB〓 reacted with carboxylic acids in DCC/DMAP/DCM system to produce ten new 5-IVB〓 esters in 66-82% yield. AVB〓 or IVB〓 also reacted with carbamino chloride or phosphoryl chloride in IM/DMAP system to produce eight corresponding carbamates or phosphorylates in good yields.

阿维菌素B〓与氨基甲酰氯反应,合成了2个5-AVB〓氨基甲酸酯衍生物:阿维菌素B〓与膦酰氯反应,合成2个5-AVB〓膦酸酯衍生物;并改进了阿维菌素与酰氯的反应条件,缩短了反应时间,提高了产率和反应的选择性。

We have studied the electrochemical oxidation reactions of bilirubin, biliverdin, bile-purpurin and choletelin in H〓O+DMF mixed solvent and found that the oxidation reactions of these bile pigments were greatly sped up by the introduction of water into DMF, and discussed the effect of water on their oxidation mechanisms too, and determined the reaction rate constants in the mixed solvent.

利用现场紫外-可见及时间分辨光谱电化学技术,研究了胆红素、胆绿素、胆汁红紫素及胆黄素在DMF+H〓O混合溶剂中的电化学氧化反应,发现由于水的引入,使上述胆汁色素在DMF中的氧化反应大大加快。研究了反应的动力学,首次求出了反应的速率常数。

A total of 129 children were enrolled in the study. Thirty-eight of the children were switched to tacrolimus monotherapy for different reasons [steroid resistant graft rejection (n = 15), chronic rejection (n = 5), severe acute rejection (n = 4), repetitive acute graft rejection (n = 5), dysfunction of the transplant (n = 3), insufficient CsA metabolism (n = 3), hypertrichosis (n = 2), and CsA toxicity (n = 1)], four patients had primary tacrolimus therapy, and 87 patients are receiving cyclosporine.

其中38名儿童因各种原因单独使用他克莫司治疗[激素型排斥反应(15例)、慢性排斥反应(5例)、严重急性排斥反应(4例)、急性重复排斥反应(5例)、移植肝失功能( 3例)、环孢素代谢不足(3例)、多毛症(2例)、环孢素毒性(1例)],4例患者使用他克莫司治疗,87例使用环孢素。

The first synthetic route uses 1,2,4-trimethoxybenzene and chloroacetonitrile in forming 2,4,5-trimethoxy-a-chlor-acetophenone under the anhydrous condition, then the intermediate condensates with papaverine forming the core pyrro[2,l-a]isoquinoline, followed by formation and lactonization to form the lactone ring. The second synthetic route uses prepared aldehyde with prepared ethyl nitroacetate by Knoevenagel condensation to obtain 2-Nitro-3-(2,4,5-tris-methoxy-phenyl)-acrylic acid ethyl ester and 2-Nitro-3-(2,4,5-tris-benzyloxy -phenyl)-acrylic acid ethyl ester etal intermediates. The lamellarin skeleton could arise from condensation of the papaverine and these intermediates by Michael reaction, the ester group is provided for subsequent lactonization. The third synthetic route uses coumarin or indan-l,3-dione derivatives and papaverine to form lamellarin under basic conditions.

第一条路线首先从1,2,4-三甲氧基苯出发与卤乙腈作用合成卤代芳酮中间体,然后与罂粟碱反应合成开链片螺素,最后经乙酰化、去保护、成内酯环得到片螺素;第二条路线由制备的芳醛和制备的硝基乙酸乙酯经缩合得到2-硝基-3-芳基丙烯酸乙酯,然后由该中间体与罂粟碱反应,在完成关环的同时也引入酯基,最后去保护、成内酯环得到片螺素;第三条路线是由香豆素或茚二酮出发,经溴代后的中间体与罂粟碱反应,得到片螺素的基本框架。

In view of the polydispersity and unhomogeneous molecular weight of soda lignin in pulping black liquor, the method which firstly classify lignin then react in homogeneous system has been adopted for a long-term to chemically modify the soda lignin, in order to improve the integral performance of lignin technical products effectively. However, there are following drawbacks in this technology: the low ultilization of lignin, and difficult seperation from the reaction system.

鉴于制浆黑液中的碱木素具有多分散性较大、分子不均一的特点,为有效提高技术木素产品的整体性能,长期以来采用先级分木素、后在均相体系中反应的方法,对碱木素进行化学改性,但此法存在木素利用率低产品难从反应相中分出的缺陷。

To test this concept in transplant recipients, we evaluated complement, complement regulator, and T cell/proinflammatory marker gene expression by quantitative real-time polymerase chain reaction in 71 archived heart transplant biopsies and correlated the results with the histologic grade of rejection. Significantly more transcripts encoding alternative pathway components factor B, C3 and properdin, and C3a receptor and C5a receptor were detected in grade 3 versus grade 0 or 1 biopsies. The grade 3 rejections also contained significantly higher amounts of CD3, interferon gamma, perforin, and granzyme B genes.

为了明确移植受者中该理论的正确性,我们采用RT-PCR的方法检测了71例心脏移植物活检标本中补体、补体调节物以及T细胞/促炎症反应标记物基因表达及其与排斥反应的组织学分级的相关程度。3级的排斥反应相比于0或者1级的排斥反应其活检标本中旁路途径成分因子B、C3以及备解素和C3a与C5a的受体表达均明显升高。3级排斥分那英同样存在更多的CD3、IFN-gamma、穿孔素和颗粒酶B基因的表达。

These enzymatic haemostatic agents can be used to antagonize the side effect of hirudin. We take the batraxobin as an example to illustrate that the enzymatic haemostatic can antagonizes hirudin. Agglutination reaction occurred after the tubes containing hirudin were added with batroxobin , i.e., batroxobin can antagonize hirudin. In a canine model,, the reduction extent of TT and APTT in the test group was larger than that in the control group; the bleeding time was decreased obviously and it was shorter in the experimental group than in the control group at lh, 2h and 3h after hirudin injection, indicating batroxobin can antagonize the bleeding side effects of hirudin.

以巴曲停为例,加入巴曲停的水蛙素抗凝试管内又可发生凝集反应,而未加入巴曲停的试管内不发生凝集反应;犬动物模型显示,水蛙素实验组TT值、 APTT值明显低于水蛙素对照组,犬给予巴曲停后出血时间明显缩短,出血时间在滴注水蛙素后lh、2h、3h明显短于对照组(P.05),说明巴曲停有拮抗水蛙素抗凝血的作用。

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