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affinity
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  亲和力
    AFFINITY BINDING OF 3H-5-HYDROXYTRYPTAMINE TO RAT BRAIN SEROTONIN RECEPTOR
    脑内5-羟色胺受体亲和力的测定
短句来源
    AFFINITY OF PENICILLIN-BINDING PROTEINS OF PSEU-DOMONAS AERUGINOSA K799/WT FOR FURBENICILLINAND OTHER ANTIPSEUDOMONAL ANTIBIOTICS
    呋苄青霉素对绿脓杆菌K799/WT青霉素结合蛋白亲和力研究
短句来源
    Affinity to α-Adrenoceptor and QSAR of Some Substituted Benzylisoquinoline
    取代苄基异喹啉化合物与α-受体的亲和力及构效关系
短句来源
    QSAR Study on α-Adrenoceptor Affinity of Some Tetrahydroisoquinoline Derivatives
    四氢异喹啉衍生物α-肾上腺素能受体亲和力的定量构效关系研究
短句来源
    Quantum Chemical Calculation and QSAR of Some Benzylisoquinoline Compounds with Affinity to α_1-Adrenoceptor
    具有α_1-受体亲和力的苄基异喹啉化合物量化计算及构效关系
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  “affinity”译为未确定词的双语例句
    CONCLUSION: The configuration of C-13a in the structural formula of p-chlorobenzyl-tetrahydroberberine might be dominant to its affinity to α1A receptor.
    结论:对氯苄基四氢小檗碱类化合物与血管α1A受体的结合能力,可能取决于结构式中C-13a的构型。
短句来源
    STUDY OF CNS RECEPTOR IMAGING AGENT(Ⅲ )── A STUDY ON THE INFLUENCE OF THE AROMATIC SUBSTITUENTS OF BENZAMIDES ON THE AFFINITY FOR DOPAMINE D_2 RECEPTOR
    中枢神经系统受体显像剂的研究(Ⅲ)──苯酰胺类多巴胺D_2受体显像剂取代基效应的研究
短句来源
    Synthesis of the Anticancer Drug with Affinity to Lymph MMC Dextran Conjugate and Studies on Its Biological Properties
    趋淋巴抗癌药丝裂霉素-右旋糖酐偶联物的合成及生物学性质的研究
短句来源
    Studies on Drug carriers with Affinity to Lymph and Prospect
    亲淋巴药物载体的研究及展望
短句来源
    Boronate affinity chromatography of antibiotics I. Study on the possibility of complexation of erythromycin and kanamycin with boric acid
    抗生素的硼酸基亲和层析 I.红霉素和卡那霉素与硼酸络合可能性的研究
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  affinity
3D-QSAR STUDIES ON SUBSTITUTED DIHYDROPYRIDINES FOR THEIR α1A-ADRENERGIC RECEPTOR BINDING AFFINITY
      
Both these models predicted binding affinity of internal and external test set compounds including the enantiomers of compound no.
      
For example, N1-(4-aminobenzenesulfonyl)-5-azaskatole (18; Ki = 41 nM) displayed an affinity comparable to N1-(4-aminobenzenesulfonyl)skatole.
      
All compounds were characterized by binding affinity determination for 5-HT2A and 5-HT2C subtypes and antagonistic activity for 5-HT2B receptor in rat stomach fundus.
      
None of the new compounds showed affinity for 5-HT2A and 5-HT2C subtypes, but some of them displayed antagonistic activity in rat stomach fundus at micromolar concentrations.
      
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(1) Sodium salt of reduced codehydrogenase I has been obtained in good yield as a dry powder from codehydrogenase I by reduction with alcohol and alcohol dehydrogenase. This preparation was stable for at least 5 months when kept dry at -15℃. (2) The properties of the particle-bound codehydrogenase I cytochrome reductase system in heart muscle preparation were found to differ considerably from those of the soluble enzyme as obtained by Mahler et al. Among other things, the affinity for cytochrome c of the...

(1) Sodium salt of reduced codehydrogenase I has been obtained in good yield as a dry powder from codehydrogenase I by reduction with alcohol and alcohol dehydrogenase. This preparation was stable for at least 5 months when kept dry at -15℃. (2) The properties of the particle-bound codehydrogenase I cytochrome reductase system in heart muscle preparation were found to differ considerably from those of the soluble enzyme as obtained by Mahler et al. Among other things, the affinity for cytochrome c of the particle-bound enzyme is much greater than the soluble enzyme. The Michaelis constant for cytochrome c of the former is only one twelfth of that of the latter.(Fig. 2A). (3) With either oxygen or excess cytochrome c as electron acceptor, it was found that the overall activity, in terms of rate of oxygen consumption or cytochrome c reduction, when both succinate and reduced codehydrogenase I were oxidized simultanously, did not represent the sum of the rates of oxidation when these two substrates were separately oxidized but equalled only the faster of the two separate oxidation rates(Fig. 5, Tables 1, 2). If 2,6-dichlorophenol indophenol was used as the electron acceptor, the overall rate of simultaneous oxidation of these two substrates was found to equal exactly the sum of the rates of separate oxidation(Table 3). (4) When either oxygen or excess cytochrome c was used as the electron acceptor, reduced codehydrogenase I and succinate each inhibited the rate of oxidation of the other(Figs 4, 6 & 7). Evidence has been presented to show that the inhibition of succinate oxidation by reduced codehydrogenase I is not due to the accumulation of oxaloacetate. (5) When malonate was also added to the reaction mixture, succinate no longer produced any inhibition of the oxidation of reduced codehydrogenase I(Fig. 8). (6) It is therefore concluded that in heart muscle preparation both succinate and reduced codehydrogenase I are oxidized by cytochrome c through a common, velocity limiting factor. This is in accordance with the view previously reached by some workers from studies on the action of certain inhibitors. However, it should be noted that in our experiments no agents which might produce any conceivable change in the colloidal structure of the enzyme system has been employed. (7) It should be emphasized that our results clearly show that great caution must be exercised in drawing conslusion on the role an enzyme might play in a complex enzyme system from studies of the properties of a solubilized enzyme. (8) It is believed that the competition of two enzyme systems for a common linking factor as demonstrated in this report has provided a new method for studies on the mutual relations of two or more enzyme systems.

(一)本報告提供了一個從輔酶Ⅰ,用酶還原法製備還原輔酶Ⅰ的方法。我們所製得的還原輔酶Ⅰ鈉鹽乾粉,可以在低温保存數月而不被氧化。 (二)與心肌製劑中顆粒相結合的輔酶Ⅰ細胞色素還原酶系,和用乙醇抽出的水溶性的輔酶Ⅰ細胞色素還原酶的性質頗不相同。其中比較重要的不同點是對於細胞色素c的親力,前者遠大於後者,其米氏常數僅約為後者的十二分之一。 (三)用一心肌顆粒製劑作為材料,無論用氧或過量之細胞色素c作為氫受體,還原輔酶Ⅰ與琥珀酸同時氧化時的總速度,不等於二者分別氧化時速度之和,而僅等於其中氧化較快者單獨氧化時之速度。但如用[2,6]二氯靛酚作為氫受體時,二者共同氧化時之總速度完全等於二者分別氧化時速度的和。 (四)當用氧或過量之細胞色素c作為氫受體時,琥珀酸與還原輔酶Ⅰ能彼此互相抑制對方氧化的速度。有足夠的實驗材料說明,還原輔酶Ⅰ對於琥珀酸氧化的抑制,不是由於草醯乙酸聚集的緣故。 (五)如果在反應混合物中同時含有琥珀酸脫氫酶的專一抑制劑,丙二酸,則琥珀酸對於還原輔酶Ⅰ氧化作用的抑制即被解除。 (六)根據以上的實驗結果,可以認為,還原輔酶Ⅰ及琥珀酸先通過一個共同的因子與細胞色素c作用。這個共同的因子在一般情形之下,也是...

(一)本報告提供了一個從輔酶Ⅰ,用酶還原法製備還原輔酶Ⅰ的方法。我們所製得的還原輔酶Ⅰ鈉鹽乾粉,可以在低温保存數月而不被氧化。 (二)與心肌製劑中顆粒相結合的輔酶Ⅰ細胞色素還原酶系,和用乙醇抽出的水溶性的輔酶Ⅰ細胞色素還原酶的性質頗不相同。其中比較重要的不同點是對於細胞色素c的親力,前者遠大於後者,其米氏常數僅約為後者的十二分之一。 (三)用一心肌顆粒製劑作為材料,無論用氧或過量之細胞色素c作為氫受體,還原輔酶Ⅰ與琥珀酸同時氧化時的總速度,不等於二者分別氧化時速度之和,而僅等於其中氧化較快者單獨氧化時之速度。但如用[2,6]二氯靛酚作為氫受體時,二者共同氧化時之總速度完全等於二者分別氧化時速度的和。 (四)當用氧或過量之細胞色素c作為氫受體時,琥珀酸與還原輔酶Ⅰ能彼此互相抑制對方氧化的速度。有足夠的實驗材料說明,還原輔酶Ⅰ對於琥珀酸氧化的抑制,不是由於草醯乙酸聚集的緣故。 (五)如果在反應混合物中同時含有琥珀酸脫氫酶的專一抑制劑,丙二酸,則琥珀酸對於還原輔酶Ⅰ氧化作用的抑制即被解除。 (六)根據以上的實驗結果,可以認為,還原輔酶Ⅰ及琥珀酸先通過一個共同的因子與細胞色素c作用。這個共同的因子在一般情形之下,也是這兩個酶系統的速度限制因子。應該指出在我們的實驗中,並未使用任何可能影響酶系統結構的條件,因此我們的結果是在一個比較接近於生理狀態的情形之下獲得的。 (七)應該着重指出,從本報告的結果可以看到,一個用人為的方法從複雜酶系上溶解下來的酶的性質,有時並不能代表這個酶在有組織的酶系統中的真實情况。 (八)我們相信,本報告所說明的兩酶系競爭一個共同因子的一些現象,將为研究複雜酶系之間的相互關係,提供一個新的方法。

The stability of synthetic phosphoramides of aniline,p-chloroaniline,p-amino- benzoic acid,o-methoxyaniline sulfanilamide and benzylamine has been tested separately in acid and alkaline(pH 5.0 and pH 9.0)solutions.It was found that all these compounds are hydrolyzed in different degrees;among which N-(p-chlorophenyl)amidophosphoric acid is the most stable.This compound was thus used as substrate for most enzyme studies in spite of its low solubility.Phosphoramides of p-aminobenzoic acid and benzylamine are unsuitable...

The stability of synthetic phosphoramides of aniline,p-chloroaniline,p-amino- benzoic acid,o-methoxyaniline sulfanilamide and benzylamine has been tested separately in acid and alkaline(pH 5.0 and pH 9.0)solutions.It was found that all these compounds are hydrolyzed in different degrees;among which N-(p-chlorophenyl)amidophosphoric acid is the most stable.This compound was thus used as substrate for most enzyme studies in spite of its low solubility.Phosphoramides of p-aminobenzoic acid and benzylamine are unsuitable as substrates,due to their instability in solution in which the enzyme activity is measured. The phosphoamidase aetivity of the purified enzyme preparation from ox spleen on the phos- phoramide compounds is higher at pH 5.0 than at pH 9.0.The rate of hydrolysis and the affinity of the enzyme with the substrate are different for different phosphoramides.It is therefore evident that phosphoamidase activity is closely related to the structure of the substrate. Among the splitting products of phosphoramides,amines have little effect on the enzyme activity,while phosphate ion has quite significant inhibitory effect. From the experiments on the enzyme activity of rat tissue ertracts,it is seen that: (1)The ratio.of the activities on substrates with similar structures is parallel in all tissues, but different in substrates with different structures,indicating that there may exist more than one phosphoamidases. (2)The content of phosphoamidase in the various tissues of the rat varies to a considerable extent.Spleen has the highest phosphoamidase content. (3)Muscle-tissue extract contains a considerable amount of phosphoamidase activity upon synthetic compounds containing P-N linkage.It would appear that phosphocreatine,which is rich in muscle,might be the natural substrate for this enzyme.

(一)磷酰胺类化合物在酸性及碱性溶液中都不稳定。在所试过的化合物中,以磷酰对氯苯胺最稳定,但它的溶解度较小。磷酰参羧基苯胺和磷酰苯甲胺的自行分解速度甚大,不过宜用为底物。 (二)牛脾部分提纯制剂在 pH5.0对于磷酰胺类化合物的活力比在 pH9.0的高。而对于不同底物的水解速度与亲和力都不相同,显示磷酸氨基酶活力与底物的结构有密切关系。在分解产物中,胺类对于该酶的活力无大影响,而磷酸根离子则有较为显著的抑制作用。(三)大鼠组织提取液对于结构相似的底物的活力之比也相似,而对于结构不同的底物,则活力之比也不相同,显示有不同磷酸氨基酶存在的可能。(四)各组织中磷酸氨基酶的含量不同,以脾脏的含量最高。(五)肌肉组织中合有磷酸氨基酶的活力,它的研究可能对于肌肉中磷酸肌酸代谢的了解有所帮助。

On the basis of testing 15 sulfonamide derivatives for diuretic actions in rats, 6-compounds [4 highly active: hydrochlorothiazide—HCT, 5-chloro-hydrochlorothiazide—HCT-55, Benzthiazide—CT-S and 3-diethylaminomethyl-hydrochlorothiazide CTo-16: one moderately active: chlorothiazide—CT; and one inactive: 3-(3',4'-dimethoxy-2'-ethyl-carboxylatephenyl)-hydrochlorothiazide—HCT-18] were chosen for comparative study on physiological dispositions in rats. A modification of the method of Baer et al. was used for the...

On the basis of testing 15 sulfonamide derivatives for diuretic actions in rats, 6-compounds [4 highly active: hydrochlorothiazide—HCT, 5-chloro-hydrochlorothiazide—HCT-55, Benzthiazide—CT-S and 3-diethylaminomethyl-hydrochlorothiazide CTo-16: one moderately active: chlorothiazide—CT; and one inactive: 3-(3',4'-dimethoxy-2'-ethyl-carboxylatephenyl)-hydrochlorothiazide—HCT-18] were chosen for comparative study on physiological dispositions in rats. A modification of the method of Baer et al. was used for the determination of these compounds in biological materials. After an oral dose of 20mg/kg, the rate of disappearance of the various compounds from the gastro-intestinal tract was found to follow the decreasing order of HCT-55, CT-S, HCT-16, HCT, CT and HCT-8. This order roughly parallels their oil-water partition coefficients with the exception of HCT-18, which was found to have the highest partition coefficient although absorbed rather slowly. CT was demonstrated to have the lowest partition coefficient which may explain its relatively slow rate of absorption from gastro-intestinal epithelium. In addition, its low pKa value (the pKa_1 of CT was found to be 6.7, while those of all other compounds investigated were between 9.0—9.2) may also affect its rate of absorption. For all compounds given orally, the highest concentrations were found in the kidneys, though three patterns of tissue distribution were observed: CT, HCT and HCT-55 were all characterized by a specific affinity for the kidney tissue and very low levels in other organs; DSA was distributed rather non-specifically in various tissues; while for CT-S and HCT-16, equally high levels were found both in the kidneys and in the liver. When given orally, the rate of excretion of the compounds in the urine was found to be essentially parallel to the rapidity of disappearance from the gastro-intestinal tract, i.e., HCT-55 > CT-S > HCT > HCT-16 > CT. After intravenous injection, nearly all of the administered dose of CT-S and HCT was found in the first five-hour urine. The percentages of urinary excretion of HCT-55, HCT-16, CT, DSA and HCT-18 were found to be 92%, 84%, 79%, 58% and 29%, respectively. The possible relationships between the characteristics of the renal transport of these compounds and their diuretic potencies are discussed in some detail.

曾观察17个双磺胺类及苯骈噻二嗪类衍生物对大鼠的利尿、排盐及排钾作用,结果表明双磺胺类作用较差;双氢氯噻嗪(HCT)类中,3位氢原子为简单基团取代的化合物(HCT-6,HCT-13,HCT-14及HCT-16)仍保留与HCT相近的利尿与排盐作用,但为芳香基取代的HCT-18卽无利尿活性,5-氯-双氢氯噻嗪(HCT-55)及Benzthiazide(CT-S)的利尿作用与HCT相等。对其中6种化合物(CT,HCT,HCT-16,CT-S,HCT-55及HCT-18)进行了在大鼠体内代谢特点的研究。发现口服后,所有这些化合物均主要以未变形式自尿排出。各化合物自胃腸道消失的速度与化合物的油/水分布系数有平行关系(HCT-18例外):HCT-55分布系数较大,吸收最快;反之,CT的分布系数最小,而且pKa值鞍低(CT的pKa_1为6.7,其他化合物的pKa_1均在9.0—9.2),吸收亦最慢。各种化合物均在腎(或肝及腎)分布最高,其他各脏均无明显堆积。口服后药物自尿的排泄速度基本上与自胃腸道消失的速度平行;静脉注射后,则以CT-S,HCT及HCT-55排泄最快,CT和DSA较慢,HCT-18最慢。本文还討論了这些化合...

曾观察17个双磺胺类及苯骈噻二嗪类衍生物对大鼠的利尿、排盐及排钾作用,结果表明双磺胺类作用较差;双氢氯噻嗪(HCT)类中,3位氢原子为简单基团取代的化合物(HCT-6,HCT-13,HCT-14及HCT-16)仍保留与HCT相近的利尿与排盐作用,但为芳香基取代的HCT-18卽无利尿活性,5-氯-双氢氯噻嗪(HCT-55)及Benzthiazide(CT-S)的利尿作用与HCT相等。对其中6种化合物(CT,HCT,HCT-16,CT-S,HCT-55及HCT-18)进行了在大鼠体内代谢特点的研究。发现口服后,所有这些化合物均主要以未变形式自尿排出。各化合物自胃腸道消失的速度与化合物的油/水分布系数有平行关系(HCT-18例外):HCT-55分布系数较大,吸收最快;反之,CT的分布系数最小,而且pKa值鞍低(CT的pKa_1为6.7,其他化合物的pKa_1均在9.0—9.2),吸收亦最慢。各种化合物均在腎(或肝及腎)分布最高,其他各脏均无明显堆积。口服后药物自尿的排泄速度基本上与自胃腸道消失的速度平行;静脉注射后,则以CT-S,HCT及HCT-55排泄最快,CT和DSA较慢,HCT-18最慢。本文还討論了这些化合物在腎脏的轉运特点与产生利尿作用之间的可能联系。本文曾经雷海鹏及金蔭昌二先生指正,特此致谢。

 
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