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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.【關鍵詞】GproteinreceptorkinasesantioxidanttempolSKFAGINGISASSOCIATEDWITHANincreaseinoxidativestressandischaracter...
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新型抗高血壓藥物-依普沙坦
...斷劑,是由史克必成公司開發,其商品名爲Teveten。別名SKF108566[1]。1藥物動力學1.1吸收依普沙坦口服後吸收迅速,富含脂質食物,減慢吸收,但不影響吸收率。生物利用度約13%,這是口服吸收不完全引起的。正常青年人血藥濃...
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ReducedrenaldopamineD1receptorfunctioninstreptozotocin-induceddiabeticrats
...tdecreaseininsulinlevelscomparedwithcontrolrats.IntravenousadministrationofSKF-38393,aD1receptoragonist,causedathreefoldincreaseinsodiumexcretionincontrolrats.However,SKF-38393failedtoproducenatriuresisindiabeticrats.SKF-38393causedaconcentration-dependentinhibitionofNa-K-ATPaseactivityinrenalproxim...
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藥物篩選技術爲遺傳疾病藥物研發提供新途徑
...KAP的表達,而IKBKAP是Riley-Day綜合症中的致病基因。其中,SKF-86466能夠通過調節細胞內PKA依賴的CREB磷酸化和cAMP水平來誘導IKBKAP轉錄,是在細胞水平上中止或逆轉疾病進程的潛在分子。Lee介紹道,這類疾病開展臨牀試驗難度較大,...
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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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山東省大學生肥胖與體質健康的關係
...褶、腹皮褶等。用迴歸方程:男身體密度=1.0977-0.00146(∑2SkF1),女:身體密度=1.0931-0.00160(∑2SkF1),其中,∑2SkF1:肱三頭肌與肩胛下角處皮褶厚度之和[2]。體脂轉化公式(Brozek公式)爲:體脂百分比=[(4.570/Db-4.142)]×100%,Db爲...
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TempolreducesoxidativestressandrestoresrenaldopamineD1-likereceptor-Gproteincouplingandfunctioninhyperglycemicrats
...關鍵詞】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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生物檢材中利血平的高效液相色譜/質譜和高效液相色譜的檢測
...定所,利血平片(石家莊市太行醫藥有限公司提供);內標:SKF525A(中國標準技術開發公司);10%鹽酸溶液;乙腈爲色譜純,其他試劑均爲分析純,水爲重蒸水。 1.2儀器與色譜條件 島津LC210ATvp高效液相色譜儀,SPD210AVvp紫外可見檢...
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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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將幹細胞應用於藥物開發
...人員很快就確定了8個化合物並進行進一步的測試,其中SKF-86466最終證明在細胞水平上能停止或逆轉疾病的進程。實驗結果的影響不只限於Riley-Day綜合徵,有許多罕見的遺傳性疾病是通過昂貴的藥物開發模式來解決的。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:有效治療乳腺癌的“組合拳”
...室的研究人員發現,達沙替尼可阻斷SFKs發送信號,沒有SKF信號,AKT就未得到“mTOR信號已被雷帕黴素關閉”的信息。因此,AKT就不知道介入並接管mTOR“發送腫瘤繼續增長的必要信號”的工作。Keri說:“我們發現,如果將這兩種...
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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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從大學到公司:高校科研的瑞典經驗
...區內,有三個國家級科學園區,同時與愛立信、沃爾沃、SKF、ABB等公司保持着良好的合作關係。奧拉·卡森(OlaCarson)是汽車工程碩士項目的負責人,他是能源工程領域的資深研究者,他告訴記者:“我們幾乎年年都會和學生們...
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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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咪唑啉類降壓藥研究新進展
...注可樂定的降壓作用下不能被NRL注射選擇性α2受體拮抗劑SKF-86466阻斷,卻能被NRL注射咪唑克生(idazoxan,含咪唑環,見上圖)完全阻斷。因此,推測可樂定很可能是作用於一種對兒茶酚胺不敏感而對咪唑啉敏感的受體起降壓作用。人...
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TheTwo-StateDimerReceptorModel:AGeneralModelforReceptorDimers
...orconcentrationsfrom0.1nMto50µM)ofnonlabeledD1dopaminereceptoragonistSKF38393(TocrisCooksonLtd.,Avonmouth,UK).Nonspecificbindingwasdeterminedinthepresenceof50µMSCH23390.Inallcases,freeandmembrane-boundligandwereseparatedbyrapidfiltrationof500-µlaliquotsinacellharvester(Brandel,Gait...