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新型抗高血压药物-依普沙坦
...断剂，是由史克必成公司开发，其商品名为Teveten。别名SKF108566［1］。1药物动力学1.1吸收依普沙坦口服后吸收迅速，富含脂质食物，减慢吸收，但不影响吸收率。生物利用度约13%，这是口服吸收不完全引起的。正常青年人血药浓...
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DesensitizationoftheDopamineD1andD2ReceptorHetero-OligomerMediatedCalciumSignalbyAgonistOccupancyofEitherReceptor
...oro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepinehydrobromide(SKF-81297)ortheD2-selectiveagonistquinpirole.DesensitizationofthecalciumsignalmediatedbyD1-D2receptorhetero-oligomerswasinitiatedbyagonistoccupancyofeitherreceptorsubtypeeventhoughthesignalwasgeneratedonlybyoccupancyofbothrec...
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DifferentialActivationofAdenylateCyclaseandReceptorInternalizationbyNovelDopamineD1ReceptorAgonists
...andbenzazepines[7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine(SKF38393),(±)-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine(SKF77434),6-chloro-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine(SKF82958),3-methyl-6-chloro-7,8-hydroxy-1-[3-methylphenyl...
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ReducedrenaldopamineD1receptorfunctioninstreptozotocin-induceddiabeticrats
...tdecreaseininsulinlevelscomparedwithcontrolrats.IntravenousadministrationofSKF-38393,aD1receptoragonist,causedathreefoldincreaseinsodiumexcretionincontrolrats.However,SKF-38393failedtoproducenatriuresisindiabeticrats.SKF-38393causedaconcentration-dependentinhibitionofNa-K-ATPaseactivityinrenalproxim...
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RenaldopamineD1receptordysfunctionisacquiredandnotinheritedinobeseZuckerrats
...pithelialcells(PTECs)fromSprague-Dawley(SD)ratstoinsulinbluntedtheabilityofSKF-38393,aD1-receptoragonist,toinhibitNKAactivity.AdecreaseinD1receptornumberanddefectivereceptor-GproteincouplingledtothefailureofSFK-38393toinhibitNKAactivityininsulin-exposedPTECs(2).Ithasbeenreportedthatrenalproximaltubu...
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Voltage-DependentBlockofN-Methyl-D-aspartateReceptorsbyDopamineD1ReceptorLigands
...alf-block,andkbisthevoltagedependenceoftheblock.Fig.1.EffectsoftheD1agonistSKF81297onNMDAreceptor(NR1A/NR2A)mediatedcurrents.A,controlresponseto100µMglutamate.B,30µMSKF81297(blackbar)significantlyinhibitedtheNMDAreceptormediatedcurrent.C,noinhibitionwasdetectedwhenSKF81297wasonlyappliedb...
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Agonist-InducedCellSurfaceTraffickingofanIntracellularlySequesteredD1DopamineReceptorHomo-Oligomer
...hendopaminewasused.Cellsweretreatedwithoneofthefollowingagonists(pergolide,SKF81297,SKF38393,apomorphine,ordopamine),antagonists(SCH23390),orinverseagonists[(+)-butaclamol,flupenthixol,orfluphenazine].RadioligandBinding.Near-maximalsaturationreceptorbindingwasdeterminedwith15to25µgofmembranepr...
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RoleofoxidativestressindefectiverenaldopamineD1receptor-GproteincouplingandfunctioninoldFischer344rats
...ultinginrestorationofD1receptor-GproteincouplingandthenatriureticresponsetoSKF-38393.Thustempol,byloweringoxidativestress,normalizestheage-relateddeclineindopaminereceptorfunction.【关键词】GproteinreceptorkinasesantioxidanttempolSKFAGINGISASSOCIATEDWITHANincreaseinoxidativestressandischaracter...
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30例严重少精症、无精子症患者的遗传学分析
...目的探讨严重少精症和无精子症与遗传因素的关系。方法260例染色体G带分析;116例Y染色体AZF区18个微缺失位点进行多重PCR基因扩增检测分析。结果30例严重少精症和无精子症患者发现遗传异常，其中26例染色体异常，4例AZF基因有...
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BooksReceived
...ainAdolescents—AFamily-BasedApproach,DanielleGrangeandJamesLock,2007,260pages,hardcover,$35.00.TheGuilfordPress,72SpringStreet,NewYork,NY10012.Internet:www.guilford.com.TheHealthImpactofSmokingandObesityandWhattoDoAboutIt,HansKrueger,DanWilliams,BarbaraKaminsky,andDavidMcLean,2007,374pages,sof...
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InvolvementofaDysfunctionalDopamine-D1/N-Methyl-D-aspartate-NR1andCa2+/Calmodulin-DependentProteinKinaseIIPathwayintheImpairmentofLatentLearni
...endentproteinkinaseII(CaMKII)inhibitor],KN92(aninactiveCaMKIIinhibitor),andSKF81297(adopamine-D1receptoragonist)werepurchasedfromSigma-Aldrich(St.Louis,MO).PCP,glycine,andSKF81297weredissolvedinsalinesolution.KN92andKN93weredissolvedina0.01%dimethylsulfoxide-containingsalinesolution.PCPwasadminister...
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药物筛选技术为遗传疾病药物研发提供新途径
...KAP的表达，而IKBKAP是Riley-Day综合症中的致病基因。其中，SKF-86466能够通过调节细胞内PKA依赖的CREB磷酸化和cAMP水平来诱导IKBKAP转录，是在细胞水平上中止或逆转疾病进程的潜在分子。Lee介绍道，这类疾病开展临床试验难度较大，...
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WorkloadDuetoAspergillusfumigatusandSignificanceoftheOrganismintheMicrobiologyLaboratoryofaGeneralHospital
...edlaboratoryandclinicalparameterswasapplied.Wefound404A.fumigatusisolatesin260patients(1/1,000microbiologylaboratorysamples;2.1patients/10,000admissions).Atotalof90isolates(22.3%)werefrompatientswithIA.Ofthe260patients,31(12%)hadinvasivedisease(IA),andtheremaining229had“nonsignificant“disease.As...
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山东省大学生肥胖与体质健康的关系
...褶、腹皮褶等。用回归方程：男身体密度=1.0977-0.00146(∑2SkF1)，女：身体密度=1.0931-0.00160(∑2SkF1)，其中，∑2SkF1：肱三头肌与肩胛下角处皮褶厚度之和［2］。体脂转化公式(Brozek公式)为：体脂百分比=［（4.570/Db-4.142）］×100%，Db为...
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TempolreducesoxidativestressandrestoresrenaldopamineD1-likereceptor-Gproteincouplingandfunctioninhyperglycemicrats
...关键词】GproteinreceptorkinasesproteinkinaseCantioxidantstreptozotocinSKFRENALDOPAMINEPLAYSANIMPORTANTroleinmaintainingsodiumhomeostasis,particularlyduringincreasesinsodiumintake.Intherenalproximaltubule,dopamineinhibitstheactivityofsodiumtransporterssuchasthesodiumhydrogenexchanger3andNa-K-ATPa...
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ReceptorRegulationofGeneExpressionofAxonGuidanceMolecules:ImplicationsforAdaptation
...oro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepinehydrobromide(SKF81297)alteredEphA5,EphrinA1,EphrinA5,andneuropilin1.cAMPandothersignaltransductionpathwaysmayregulategeneexpressionofaxonguidancemolecules,potentiallylinkingmonoaminereceptoractivationtosignaltransductioncascades,transcrip...
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ActivationofdopamineD1-likereceptorsinducesacuteinternalizationoftherenalNa+/phosphatecotransporterNaPi-IIainmousekidneyandOKcells
...atedkidneysliceswiththeselectiveD1-likereceptoragonistsfenoldopam(10μM)andSKF-38393(10μM)for1hinducedNaPi-IIainternalizationandreducedexpressionofNaPi-IIainthebrushbordermembrane(BBM).TheD2-likeselectiveagonistquinpirole(1μM)hadnoeffect.TheD1andD2agonistsdidnotaffecttherenalNa+/sulfatecotransport...
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用核酸序列分析鉴别甲肝病毒疫苗株与野毒株
...验动物中心，公母各一，编号103，106，猴龄2～3岁，体重260～350克。感染前经检测血清抗-HAV阴性，ALT、AST、ICD等肝脏酶活性和肝组织病理检查均正常。该品系狨猴对甲肝病毒感染的敏感性高，是研究甲肝病毒可靠动物模型〔4〕...
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生物检材中利血平的高效液相色谱/质谱和高效液相色谱的检测
...定所，利血平片(石家庄市太行医药有限公司提供);内标：SKF525A(中国标准技术开发公司);10%盐酸溶液;乙腈为色谱纯，其他试剂均为分析纯，水为重蒸水。 1.2仪器与色谱条件 岛津LC210ATvp高效液相色谱仪，SPD210AVvp紫外可见检...
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ComparisonoftotalbodypotassiumwithothertechniquesformeasuringleanbodymassinmenandwomenwithAIDSwasting
...(DXA),bioelectricalimpedanceanalysis(BIA),andskinfold-thicknessmeasurement(SKF)in132patients(63men,69women)withAIDSwasting(weight90%ofidealbodyweight,orweightloss10%oforiginal,orboth).Noneofthesubjectsexhibitedclinicallipodystrophy.ComparisonsweremadebyusingdifferentBIAequations.Results:Leanbodymass...
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将干细胞应用于药物开发
...人员很快就确定了8个化合物并进行进一步的测试，其中SKF-86466最终证明在细胞水平上能停止或逆转疾病的进程。实验结果的影响不只限于Riley-Day综合征，有许多罕见的遗传性疾病是通过昂贵的药物开发模式来解决的。作者：
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p38MAPkinaseinhibitionamelioratescisplatinnephrotoxicityinmice
...reaseininfiltratingleukocytes.However,animalstreatedwiththep38MAPKinhibitorSKF-86002alongwithcisplatinshowedlessrenaldysfunction(BUN:55±14mg/dl,creatinine:0.3±0.02mg/dl,P<0.05),lessseverehistologicaldamage,andfewerleukocytescomparedwithcisplatin+vehicle-treatedanimals.SerumlevelsofTNF-,sTNFRI,ands...
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沙芬伪麻咀嚼片
...加入十二烷基硫酸钠2.0g和磷酸1.0ml为流动相，检测波长为260nm，理论板数按盐酸伪麻黄碱计算，应不低于2000；盐酸伪麻黄碱和氢溴酸右美沙芬的分离度均应符合要求。测定法精密称取氢溴酸右美沙芬对照品15mg及经105℃干燥至恒...
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AnalyticalVerificationofaPCRAssayforIdentificationofBordetellaavium
...aviumchromosomalDNA,rangingfrom25pgto1,300pg,wasestimatedtobebetween25pgand260pg(K.B.Register,unpublisheddata).TheeffectsofalteringtheconcentrationofDMSO,MgCl2,orprimersonproductyieldofPCRscontainingtemplateamountswithinthisrangewerenextcompared.Optimalconcentrationswereidentifiedas5%DMSO,0.5μMprim...
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HPLC法测定苦玄参中苦玄参苷IA的含量
【摘要】目的建立苦玄参药材PicriafelterraeLour.的含量测定方法。方法RP-HPLC法，采用C18ODS2柱(5μm，4.6×250mm)，乙腈-0.3%磷酸(34∶66)为流动相,流速为1ml/min，检测波长为264nm。结果苦玄参苷IA进样量在0.42～2.10μg的范围内呈良好的线性...
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辛伐他汀片
...液，照分光光度法（中国药典1995年版二部附录IVA），于260～210nm的波长范围内测定吸收度，在247、238与231nm的波长处有最大吸收。（2）在含量测定项下记录的色谱图中，供试品峰的保留时间应与对照品峰的保留时间一致。 检...
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第二节 MHC抗原的结构及检测
...方块表示尚未确定的多肽折叠。 2.I区相关抗关 (1)Ia抗原的概念:Klein、Shrefler(1974、1975年)将小鼠I区基因所编码的抗原称为Ia抗原(Iregionassociatedantigen)，也有人将I区中的Ir基因的产物称为Ia抗原。目前一般把人类Ⅱ类抗原，尤...
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胰岛β细胞自身抗体IA-2Ab的ELISA方法建立——附110例正常人测定值
....4P.294-2969（天津）为了以本实验室研制的重组人自身抗原IA-2作为抗原，建立血清中抗IA-2的自身抗体的ELISA测定方法，并对正常人群进行检测。研究者在间接ELISA法建立过程中对封闭剂、血清稀释度及二抗稀释度及其他测试条件进...
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糖尿病相关胰岛自身抗体检测的临床意义
...（ICA）、谷氨酸脱羟酶抗体（GADA）、胰岛素自身抗体（IAA）、以及蛋白酪氨酸磷酸酶抗体（IA-2A）等四种抗体的临床意义较大。本文复习了近年文献报道的一些结果。 1检测方法的完善与标准化 ICA检测是临床上应用较早...
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CT和PET：Ia期肺癌诊断分期偏低
...eting.2008May10-14医学空间（MEDcyber.com）7月3日消息-临床分期Ia期非小细胞肺癌目前倾向于缩小切除范围。这一治疗策略依赖于临床分期的准确，这依赖于影像学检查技术。纽约的Brendon等研究考察了CT和PET在患者临床分期的准确性，...