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活性代谢物     
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  active metabolite
     Both Vitamin D_3 active metabolite 25-OH-D_3 and 1,25-(OH)_2-D_3 play improtant role in animal and poultry nutrition.
     维生素D3及其活性代谢物25-羟基D3和1,25-羟基D3对畜禽营养具有很重要的意义。
短句来源
     CONCLUSION: Cytotoxicity of flutamide and its effect on CYP1A2 mRNA were stronger than those of its active metabolite 2-hydroxyflutamide in primary rat hepatocytes.
     结论:氟他胺对原代培养大鼠肝细胞的毒性大于其活性代谢物2-羟基氟他胺,且明显增加CYP1A2 mRNA水平.
短句来源
     Determination of leflunomide's active metabolite A_(771726) in human serum by RP-HPLC
     反相高效液相色谱法测定血清中来氟米特活性代谢物A_(771726)的浓度
短句来源
     Pharmacokinetics of active metabolite of suplatast tosilate(M-1) in healthy volunteers
     甲磺司特活性代谢物M-1的人体药代动力学
短句来源
     Method 5 THP-1 monocytes were exposed to different levels of Tam or OH-Tam (an active metabolite of Tam) for 24hrs and then the surface expression of CD36 was analyzed.
     方法 分别以不同浓度Tam(1,5,10 μmol/L)和它的活性代谢物羟-三苯氧胺(OH-Tam)作用于培养的THP-1单核细胞,24 h后观察CD36蛋白在细胞表面的表达;
短句来源
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  bioactive metabolite
     Objective:To establish a quick HPLC method for determination of bioactive metabolite Mycophenolic acid(MPA) of Mycophenolate mofetil (MMF) in human plasma.
     目的:建立快速测定肾脏移植血浆中麦考吗乙酯(Mycophenolate mofetil,MMF)活性代谢物霉酚酸(Mycophenolic ac id,MPA)的高效液相色谱测定方法。
短句来源
     Objective:To rapidly establish a HPLC method for the determination of bioactive metabolite fenofibric acid of fenofibrate in human plasma.
     目的 :建立快速测定人血浆中非诺贝特活性代谢物非诺贝酸 (fenofibricacid)的高效液相色谱方法。
短句来源
     A HPLC method for the rapid determination of mycophenolic acid, bioactive metabolite of mycophenolate mofetil, in human plasma had been developed.
     建立人血浆中麦考酚酸酯活性代谢物麦考酚酸的 HPL C测定法。
短句来源
     OBJECTIVE To establish an HPLC method for the determination of bioactive metabolite acyclovir of valaciclovir in human plasma.
     目的:建立人血浆中伐昔洛韦活性代谢物阿昔洛韦的高效液相色谱测定法。
短句来源
  active metabolites
     OBJECTIVE To establish a simple HPLC method for the simultaneous determination of primidone (PRI), lamotrigen (LTG), phenobarbital (PB), phenytoin(PHT), oxcarbazepine (OXC), carbamazepine(CBZ) and two active metabolites of monohydroxycar bazepine (MHD), carbamazepine 10,11-epoxide(CBZE) in human plasma.
     目的建立了同时测定人血浆中扑米酮(PRI)、拉莫三嗪(LTG)、苯巴比妥(PB)、苯妥英(PHT)、奥卡西平(OXC)、卡马西平(CBZ)及两种活性代谢物单羟奥卡西平(MHD)、环氧卡马西平(CBZE)浓度的HPLC方法。
短句来源
     Determination of Analginum and Its Main Active Metabolites in Rabbit Plasma by RP-HPLC
     RP─HPLC法测定兔血浆中安乃近及其活性代谢物的浓度
短句来源
     METHODS: The oseltamivir and it's active metabolites concentration in plasma were determined by HPLC fluorescence method.
     方法 :采用反相高效液相色谱 荧光检测法测定血浆中奥司他韦及其活性代谢物的浓度。
短句来源
     These observations showed that one of the active metabolites of amiprophos in vivo might be H2S whichwas responsible for the loss of P450. Although high dose of amiprophos destroyed P450 in vivo as well as in vitro, lower dose (e. g. 0.lg/kg) and shorter term exposure would not induce rats to develop hepatotoxicity characterized by the loss of P450.
     此现象似提示消草磷的体内活性代谢物之一或许是硫化氢。 尽管高剂量消草磷体内与体外均导致P450破坏,但低剂量(如 0.1g/kg)短期接触却不致诱发以肝脏P450丢失为特征的特殊肝脏毒性。
短句来源
     Conclusion Drug sera from rats per os Da Cheng Qi granules of various concentrations are able to make mice IELs produce/secrete IL-2, this effect may relate to the action of Da Cheng Qi granules and components and their active metabolites and/or induced intrinsic substances induced by them.
     结论:不同浓度的大承气颗粒制备的药物血清具有使IEL产生/分泌IL-2的作用; 该作用涉及到药物本身和药物在体内的活性代谢物和/或其诱导的内源性活性物质的作用。
短句来源
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  its active metabolite
     CONCLUSION: Cytotoxicity of flutamide and its effect on CYP1A2 mRNA were stronger than those of its active metabolite 2-hydroxyflutamide in primary rat hepatocytes.
     结论:氟他胺对原代培养大鼠肝细胞的毒性大于其活性代谢物2-羟基氟他胺,且明显增加CYP1A2 mRNA水平.
短句来源
     A rapid and simultaneous high performance liquid chromatographic (HPLC) method for the determination of cryptotanshinone (CT) and its active metabolite Tanshinone ⅡA (Ts ⅡA) in porcine plasma has been validated.
     本试验建立了用反相HPLC同时进行猪血浆中隐丹参酮(CT)及其活性代谢物丹参酮ⅡA(Ts-ⅡA)的快速定量检测方法。
短句来源
     Objective:To establish a rapid and feasible HPLC method for the determination of mycophenolate mofetil (MMF) and its active metabolite mycophenolic acid(MPA) in human plasma.
     目的:建立快速测定人血浆中霉酚酸酯(mycophenolate mofetil,MMF)及其活性代谢物霉酚酸(mycophenolic acid,MPA)浓度的高效液相色谱方法。
短句来源
     Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects
     氯雷他定及其活性代谢物去羧乙氧基氯雷他定在中国健康受试者的药动学(英文)
短句来源
     Determination of tramadol and its active metabolite O-desmethyltramadol in plasma and amniotic fluid using LC/MS/MS
     LC/MS/MS法测定血浆、羊水中曲马多及其活性代谢物氧去甲基曲马多
短句来源
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  active metabolite
The pharmacokinetics of α- and β-diastereomers of Arteether, a well-known antimalarial drug and its active metabolite dihydroartemisinin (DHA) were studied in Sprague-Dawley rats, Rhesus monkeys and human volunteers.
      
When the blood level of the active metabolite of vitamin D3 was set to one-tenth of its norm, the rate of compact bone resorption changed only slightly.
      
The results indicated that AtRA, an active metabolite of vitamin A, affected germ cell and gonad development of embryos and the larvae of giant freshwater prawn.
      
Since 1αOhase can locally convert 25-hydroxyvitamin D into 1α,25-dihydroxyvitamin D (1,25(OH)2D), an active metabolite of vitamin D, it is suggested that local production of 1,25(OH)2D by macrophages may promote atherosclerotic calcification.
      
Capillary electrophoresis with an electrolyte containing cyclodextrin was investigated for the simultaneous separation of the diastereoisomers of 6R,S-leucovorin and its active metabolite 6R,S-5-methyl-tetrahydrofolate.
      
更多          
  bioactive metabolite
We also measured plasma levels of guanosine 3'∶5'-cyclic monophosphate (cyclic GMP) as SIN 1, the bioactive metabolite of molsidomine, becomes effective via activation of soluble guanylate cyclase.
      
Mycophenolic acid (MPA) is the bioactive metabolite of MMF.
      
Biological effects of tolytoxin (6-hydroxy-7-O-methyl-scytophycin b), a potent bioactive metabolite from cyanobacteria
      
Lisinopril (MK521), a lysine analogue of enalaprilic acid, the bioactive metabolite of enalapril, has a longer half-life than enalaprilic acid, and is excreted unchanged in the urine.
      
CYP72A2 gene mediated resistance suggests that the plant-pest or -pathogen interactions may have been modified by changes in bioactive metabolite pools.
      
更多          
  active metabolites
Significant (p?=?0.0061) increases of radioactivity were observed in kidney, spleen, and thyroid, which could be exampled by the effects of the extract and/or by the generation of active metabolites.
      
Fungi in sediments of the sea of Japan and their biologically active metabolites
      
Antibacterially active metabolites were not detected with only two of 12 penicillins, namely amoxicillin and mezlocillin.
      
The measurements were compared by linear distribution independent regression, and were found to be equivalent, indicating no major antimicrobially active metabolites of HR 810.
      
The measurements obtained were compared by linear distribution independent regression, and were found to be equivalent, indicating no major antimicrobially active metabolites of cefpirome.
      
更多          
  its active metabolite
The pharmacokinetics of α- and β-diastereomers of Arteether, a well-known antimalarial drug and its active metabolite dihydroartemisinin (DHA) were studied in Sprague-Dawley rats, Rhesus monkeys and human volunteers.
      
Capillary electrophoresis with an electrolyte containing cyclodextrin was investigated for the simultaneous separation of the diastereoisomers of 6R,S-leucovorin and its active metabolite 6R,S-5-methyl-tetrahydrofolate.
      
A new liquid chromatographic method with columnswitching has been developed for the simultaneous determination of losartan and its active metabolite, EXP3174 in rat plasma.
      
Automated microbore LC with peak compression for the assay of GR138950 and its active metabolite in human serum
      
The advantages of this approach were clearly illustrated in the automated, microbore LC-peak compression assay of GR138950, a novel non-peptide angiotensin II antagonist selective for the AT1 receptor and its active metabolite in human serum.
      
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  其他


After incubation of amiprophos (O-ethyl-O- (2-nitro-4 methylphenyl)-N-isopropyl thiono phosphoroamide) with liver microsomesof rats pretfeated with phenobarbital (PB) in the presence of NADPH, 58% of the microsomal cytochrome P450 would be lost at most. 18 h after ip or po l.0g/kg amiprophos, the microsomal P450 of PB pretreated rats decreased to 60% of control value, but the composition of subpopulations of P450 showed no significant change as estimated by the production of the complex compound of reduced form...

After incubation of amiprophos (O-ethyl-O- (2-nitro-4 methylphenyl)-N-isopropyl thiono phosphoroamide) with liver microsomesof rats pretfeated with phenobarbital (PB) in the presence of NADPH, 58% of the microsomal cytochrome P450 would be lost at most. 18 h after ip or po l.0g/kg amiprophos, the microsomal P450 of PB pretreated rats decreased to 60% of control value, but the composition of subpopulations of P450 showed no significant change as estimated by the production of the complex compound of reduced form of P450 and mety rapone. These observations showed that one of the active metabolites of amiprophos in vivo might be H2S whichwas responsible for the loss of P450. Although high dose of amiprophos destroyed P450 in vivo as well as in vitro, lower dose (e. g. 0.lg/kg) and shorter term exposure would not induce rats to develop hepatotoxicity characterized by the loss of P450.

消草磷与经苯巴比妥预处理大鼠的肝微粒体一起温育,在有NADPH存在时,最多可使肝微粒体细胞色素P450丢失58%左右。苯巴比妥预处理大鼠经ip或po 1.0g/kg消草磷,18h后肝微粒体P450将丢失40%左右,但用还原态P450甲吡酮络合物生成量估算剩余P450的亚族组成却无显著变化。此现象似提示消草磷的体内活性代谢物之一或许是硫化氢。尽管高剂量消草磷体内与体外均导致P450破坏,但低剂量(如 0.1g/kg)短期接触却不致诱发以肝脏P450丢失为特征的特殊肝脏毒性。

This paper deals with the formulation, preparation, dissolution and pharmacokinetics of a sustained release procainamide hydrochloride (PA. HCI) tablet——an oral osmotic pump(B). The orifice of B was prepared by a developed laser machine.A dual wavelength UV spectrophotometric method for the determination of PA was established. PA and its active metabolite N-acetylprocainamide(NAPA) in serum or saliva were separated and detected by a modified HPLC method. The pharmacokinetic parameters were fitted by nonlinear...

This paper deals with the formulation, preparation, dissolution and pharmacokinetics of a sustained release procainamide hydrochloride (PA. HCI) tablet——an oral osmotic pump(B). The orifice of B was prepared by a developed laser machine.A dual wavelength UV spectrophotometric method for the determination of PA was established. PA and its active metabolite N-acetylprocainamide(NAPA) in serum or saliva were separated and detected by a modified HPLC method. The pharmacokinetic parameters were fitted by nonlinear least square method with a computer on the basis of two-compartment model. The results showed that the osmotic pump tablet released drug with a zero-order kinetic, and a significant correlation was found between in vitro dissolution and in vivo absorption. The pharmacokineticpharmacodynamie data suggested a good relationship between the drug concentrations in serum or saliva and therapeutic effects.

本文研究了盐酸普鲁卡因胺(PA·HCl)渗透泵片的处方组成、制备工艺、体外溶出;建立了PA·HCl的紫外双波长分光光度法及血清和唾液中PA及其活性代谢物N-乙酰普鲁卡因胺(NAPA)共存下的高效液相色谱法,体内PA实验数据按双室模型,用电子计算机处理求得药动学参数。药动学—药效学数据显示血药浓度和唾药浓度均与药效变化规律相关。

The pharmacokinetics of 5- fluorouracil (5-FU) was studied in 7 patients with neoplastic disease who received iv infusion of 5-FU. 5-FU concentrations were measured in serum by high performance liquid chromatography (HPLC). Serum concentrations of 5 -FU .were fitted a one-compartment open model adequately, The pharmacokinetic parameters were found to be: T1/2, 14.82 min; V, 1.3528 L/kg; Cl, 0.0728 L/min.kg; and AUC, 121.25 mg. min/L. We have attempted to measure mesenteric and systemic drug concentrations in...

The pharmacokinetics of 5- fluorouracil (5-FU) was studied in 7 patients with neoplastic disease who received iv infusion of 5-FU. 5-FU concentrations were measured in serum by high performance liquid chromatography (HPLC). Serum concentrations of 5 -FU .were fitted a one-compartment open model adequately, The pharmacokinetic parameters were found to be: T1/2, 14.82 min; V, 1.3528 L/kg; Cl, 0.0728 L/min.kg; and AUC, 121.25 mg. min/L. We have attempted to measure mesenteric and systemic drug concentrations in 12 patients following rectal administration of 5-FU, and the results were listed in table 3. Metabolite 5- fluoro - 2' - deoxyuridine (FUdR) was not detected in all 19 patients who received 5-FU.

本文应用高效液相色谱法测定血药浓度,对7例肿瘤患者静脉滴注5—氟尿嘧的药代动力学进行了研究。结果表明5—氟尿嘧啶在体内衰减呈一室开放模型,T2/1为14.82min,(?)为13(?)28L/kg,(?)为0.0728L/min.kg,AUC为121.25mg.min/L。本文还研究了12例肿瘤患者直肠给药后5—氟尿嘧啶在不同部位血清中分布情况,结果见表3。全部19例患者的血清中均测不到5—氟尿嘧啶的活性代谢物5—氟脱氧尿苷。

 
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