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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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Agonist-InducedCellSurfaceTraffickingofanIntracellularlySequesteredD1DopamineReceptorHomo-Oligomer
...hendopaminewasused.Cellsweretreatedwithoneofthefollowingagonists(pergolide,SKF81297,SKF38393,apomorphine,ordopamine),antagonists(SCH23390),orinverseagonists[(+)-butaclamol,flupenthixol,orfluphenazine].RadioligandBinding.Near-maximalsaturationreceptorbindingwasdeterminedwith15to25µgofmembranepr...
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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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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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RoleofoxidativestressindefectiverenaldopamineD1receptor-GproteincouplingandfunctioninoldFischer344rats
...ultinginrestorationofD1receptor-GproteincouplingandthenatriureticresponsetoSKF-38393.Thustempol,byloweringoxidativestress,normalizestheage-relateddeclineindopaminereceptorfunction.【关键词】GproteinreceptorkinasesantioxidanttempolSKFAGINGISASSOCIATEDWITHANincreaseinoxidativestressandischaracter...
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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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ReducedrenaldopamineD1receptorfunctioninstreptozotocin-induceddiabeticrats
...tdecreaseininsulinlevelscomparedwithcontrolrats.IntravenousadministrationofSKF-38393,aD1receptoragonist,causedathreefoldincreaseinsodiumexcretionincontrolrats.However,SKF-38393failedtoproducenatriuresisindiabeticrats.SKF-38393causedaconcentration-dependentinhibitionofNa-K-ATPaseactivityinrenalproxim...
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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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RenaldopamineD1receptordysfunctionisacquiredandnotinheritedinobeseZuckerrats
...pithelialcells(PTECs)fromSprague-Dawley(SD)ratstoinsulinbluntedtheabilityofSKF-38393,aD1-receptoragonist,toinhibitNKAactivity.AdecreaseinD1receptornumberanddefectivereceptor-GproteincouplingledtothefailureofSFK-38393toinhibitNKAactivityininsulin-exposedPTECs(2).Ithasbeenreportedthatrenalproximaltubu...
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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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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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ChemotherapyCompoundsinCervicalCancerCellsPrimedbyReconstitutionofp53FunctionafterShortInterferingRNA-MediatedDegradationofHumanPapillomavi
...tedagainstHPV16E6mRNA(16E6-191siRNA),HPV18E6mRNA(18E6-165,18E6-340,and18E6-385siRNAs)andHPV18E7mRNA(18E7-604and18E7-694siRNAs).Thetargetsequenceof18E6-165siRNAissharedbybothE6andE6transcripts,whereasthetargetsequencesof18E6-385and18E6-340siRNAsarepresentonlyintheunsplicedE6/E7mRNA(Table1).Inthecours...
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大学生神经衰弱385例综合治疗疗效分析
...精神痛苦,而且影响工作、学习、生活。采用综合疗法对385例大学生神经衰弱患者进行了治疗,现将疗效分析如下。 1临床资料 1.1病例选择 按中华医学会精神科分会中国精神障碍分类与诊断标准第3版(简称CCMD-3)神...
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肠梗阻385例临床分析
...0年来肠梗阻的诊治经验。方法回顾性分析了10年间收治的385例肠梗阻资料。结果病因明确335例(87%),其中机械性肠梗阻338例(87.8%)。非手术治疗235例(61.0%),手术治疗150例(39%),术后并发症6例(4%),死亡16例(10.7%)。...
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散寒解毒、行气化瘀方药内服结合灌肠治疗慢性盆腔炎385例临床观察
...气化瘀方药内服结合灌肠治疗慢性盆腔炎的疗效。方法将385例患者分为治疗组193例,对照组192例;治疗组给予散寒解毒、行气化瘀方药内服和灌肠治疗,对照组单纯内服散寒解毒、行气化瘀方药。疗程均为30天。结果治疗组总有...
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绝经后阴道出血385例分析
...。方法我们对1998年4月~2004年4月我院门诊与病房诊治的385例PMB患者进行了临床与病理分析。结果资料显示导致绝经后阴道出血的病因可分为三大类:良性疾病占52.67%,非器质性疾病占24.61%,恶性肿瘤占22.72%。结论在绝经后早期定...
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妇科急症385例临床分析
我们自2000年4月30日~2004年4月30日共行妇科急症手术385例。占同期妇科手术的16.3%,现就其诊断和鉴别诊断做回顾性总结如下。 1临床资料1.1一般资料自2000年4月30日~2004年4月30日共行妇科急症手术385例,发病年龄13~58岁,平...
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血尿酸浓度与胰岛素抵抗的相关性研究(对385例高尿酸血症患者的临床统计分析)
...讨高尿酸血症与胰岛素抵抗的相关性。方法观察并统计了385例高尿酸血症患者的高血压(HBP)、糖尿病/IGT(DM/IGT)、冠心病(CHD)、脑血管意外(Stroke)的发病情况,同时检测了他们的血尿酸浓度(UA)、血浆甘油三酯(TG)、...
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InvolvementofDopamineSysteminRegulationofNa+,K+-ATPaseintheStriatumuponActivationofOpioidReceptorsbyMorphine
...dfromMerck(Darmstadt,Germany).Naltrexone,db-cAMP,H-89,SCH23390,eticlopride,SKF38393,quinpirole,3-isobutyl-1-methylxanthine,andouabainweresuppliedbySigmaChemicalCo.(St.Louis,MO).AnimalsandMorphineTreatment.Kunmingstrainmalemice(25-30g)wereobtainedfromtheLaboratoryAnimalCenter,ChineseAcademyofSciences...
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NorovirusesasaCauseofTraveler‘sDiarrheaamongStudentsfromtheUnitedStatesVisitingMexico
...idregionoftargetviralgenomewereusedasdescribedpreviously(17).Briefly,theG1-SKF/G1-SKRandG2-SKF/G2-SKRprimersetswereusedforamplifyingNoVgenotypesIandII(GIandGII,respectively),generatinga330-bpanda344-bpPCRproduct,respectively.TheQIAGENone-stepreversetranscriptasePCR(RT-PCR)kit(QIAGEN,Valencia,CA)wast...
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InsightsintotheCholecystokinin2ReceptorBindingSiteandProcessesofActivation
...ECL1)andinteractedwiththeimidazolegroupofHis381(H7.39)andthephenylringofTyr385(H7.43).Mutagenesisandpharmacologicalstudiesvalidatedtheseinteractions.ItisnoteworthythatthemutationofPhe120toTrpconferredconstitutiveactivitytotheCCK2R.Molecularmodelingandexperimentalworksidentifiedtheresiduesinvolvedint...
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第385次香山科学会议聚焦自组装本质规律研究
...“功能超分子体系:多层次的分子组装体为主题的第385次香山科学会议的中外专家指出,揭示自组装的本质和规律是当前自组装研究的迫切需求;尽管国内外自组装的研究取得了较快发展,但依然有许多问题亟待研究。构建...
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IdentificationofEssentialHistidineandCysteineResiduesoftheH+/OrganicCationAntiporterMultidrugandToxinExtrusion(MATE)
...ineresiduesofrat(r)MATE1conservedamongspeciesweremutated,substitutionofHis-385,Cys-62,andCys-126ledtoasignificantlossoftetraethylammonium(TEA)transportactivity.CellsurfacebiotinylationandimmunofluorescenceanalyseswithconfocalmicroscopyindicatedthatrMATE1mutantproteinswerelocalizedatplasmamembranes.M...
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Cyclooxygenases,microsomalprostaglandinEsynthase-1,andcardiovascularfunction
...hievingamorethan95%meaninhibitionofplateletTXformation(13),andmutantPGHS-2Y385Fmice,inwhichtheCOX,butnottheperoxidase(POX),functionoftheenzymeisinactivated,therebymimickingtheeffectofaselectivePGHS-2inhibitor(14).WhileTXMismarkedlydepressedbyPGHS-1knockout(KO)orKD,itisnotalteredsignificantlyinPGHS-2...
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CancerRes:有效治疗乳腺癌的“组合拳”
...室的研究人员发现,达沙替尼可阻断SFKs发送信号,没有SKF信号,AKT就未得到“mTOR信号已被雷帕霉素关闭”的信息。因此,AKT就不知道介入并接管mTOR“发送肿瘤继续增长的必要信号”的工作。Keri说:“我们发现,如果将这两种...