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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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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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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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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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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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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...
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RosiglitazonerestoresrenalD1Areceptor-Gsproteincouplingbyreducingreceptorhyperphosphorylationinobeserats
...dthatnatriureticresponsetoexogenouslyinfuseddopamineD1-likereceptoragonist,SKF-38393,isreducedininsulin-resistantobeseZuckerrats(26).ThisimpairednatriureticresponsetoSKF-38393iscausedbyinsulinresistance,becausetreatmentoftheseanimalswithaninsulin-sensitizingdrug,rosiglitazone,restoredtheabilityofSKF...
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Responseofdescendingvasarectatoluminalpressure
...YT25mmHg.TheremovalofextracellularCa2+andblockadebyeitherLa3+(10µM)orSKF-96365(100µM)eliminatedtheresponse.Luminalpressurizationto25mmHgincreasednitricoxide(NO)generation,aresponseblockedbyNOsynthaseinhibitionorremovalofextracellularCa2+.TheNOgenerationwasnotaffectedbythesuperoxidedismut...
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PharmacologicalCharacterizationandMolecularDeterminantsoftheActivationofTransientReceptorPotentialV2ChannelOrthologsby2-AminoethoxydiphenylBo
...[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl)-1H-imidazolehydrochloride(SKF96365),twopotassiumchannelblockers,tetraethylammonium(TEA)and4-aminopyridine,andaninhibitorofcapacitativecalciumentry,1-(2-(trifluoromethyl)phenyl)imidazole(TRIM),werefoundtoinhibitTRPV2activationby100µM2APB.Activati...
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InVivoRegulationofHomer1aExpressionintheStriatumbyCocaine
...ls.Cocainehydrochloride,Gö6983,phorbol12-myristate13-acetate,dopamine,SKF82958,eticlopride,8-bromo-cAMP,andKN62werepurchasedfromSigma(St.Louis,MO).QuinpiroleandSCH23390werepurchasedfromTocrisCooksonInc.(Ballwin,MO).H89andRo-31-8220werepurchasedfromCalbiochem(SanDiego,CA).Statistics.Theresultsar...
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MolecularEpidemiologyofCalicivirusesDetectedinSporadicandOutbreakCasesofGastroenteritisinFrancefromDecember1998toFebruary2004
...thercharacterizedbysequencinginthecapsidgeneusingprimersSRI-1/SRI-2(13)orG1SKF/G1SKR(19)forgenogroupI(GI)andMon381/Mon383(26)orG2SKF/G2SKR(19)forgenogroupII.Inaddition,somegenogroupIstrainswhichwereweaklyamplifiedornotamplifiedinthepolymerasegeneweredetectedandwerethusalsocharacterizedbyamplificatio...
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从大学到公司：高校科研的瑞典经验
...区内，有三个国家级科学园区，同时与爱立信、沃尔沃、SKF、ABB等公司保持着良好的合作关系。奥拉·卡森（OlaCarson）是汽车工程硕士项目的负责人，他是能源工程领域的资深研究者，他告诉记者：“我们几乎年年都会和学生们...
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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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Gi3protein-coupleddopamineD3receptor-mediatedinhibitionofrenalNHE3activityinSHRproximaltubularcellsisaPLC-PKC-mediatedevent
...SB-203580,andU-73122werepurchasedfromSigma.R-(+)-7-Hydroxy-DPAT(7-OH-DPAT),SKF-83566hydrochloride,(±)-SKF-38393hydrochloride,andS(-)-sulpiridewereobtainedfromResearchBiochemicalsInternational.Acetoxymethylesterof2‘,7‘-bis(carboxyethyl)-5(6)-carboxyfluorescein(BCECF-AM),fura2,andnigericinw...
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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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咪唑啉类降压药研究新进展
...注可乐定的降压作用下不能被NRL注射选择性α2受体拮抗剂SKF-86466阻断，却能被NRL注射咪唑克生(idazoxan,含咪唑环，见上图)完全阻断。因此，推测可乐定很可能是作用于一种对儿茶酚胺不敏感而对咪唑啉敏感的受体起降压作用。人...
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TheTwo-StateDimerReceptorModel:AGeneralModelforReceptorDimers
...orconcentrationsfrom0.1nMto50µM)ofnonlabeledD1dopaminereceptoragonistSKF38393(TocrisCooksonLtd.,Avonmouth,UK).Nonspecificbindingwasdeterminedinthepresenceof50µMSCH23390.Inallcases,freeandmembrane-boundligandwereseparatedbyrapidfiltrationof500-µlaliquotsinacellharvester(Brandel,Gait...