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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.【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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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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大學生神經衰弱385例綜合治療療效分析
...精神痛苦,而且影響工作、學習、生活。採用綜合療法對385例大學生神經衰弱患者進行了治療,現將療效分析如下。 1臨牀資料 1.1病例選擇 按中華醫學會精神科分會中國精神障礙分類與診斷標準第3版(簡稱CCMD-3)神...
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腸梗阻385例臨牀分析
...0年來腸梗阻的診治經驗。方法回顧性分析了10年間收治的385例腸梗阻資料。結果病因明確335例(87%),其中機械性腸梗阻338例(87.8%)。非手術治療235例(61.0%),手術治療150例(39%),術後併發症6例(4%),死亡16例(10.7%)。...
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散寒解毒、行氣化瘀方藥內服結合灌腸治療慢性盆腔炎385例臨牀觀察
...氣化瘀方藥內服結合灌腸治療慢性盆腔炎的療效。方法將385例患者分爲治療組193例,對照組192例;治療組給予散寒解毒、行氣化瘀方藥內服和灌腸治療,對照組單純內服散寒解毒、行氣化瘀方藥。療程均爲30天。結果治療組總有...
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絕經後陰道出血385例分析
...。方法我們對1998年4月~2004年4月我院門診與病房診治的385例PMB患者進行了臨牀與病理分析。結果資料顯示導致絕經後陰道出血的病因可分爲三大類:良性疾病佔52.67%,非器質性疾病佔24.61%,惡性腫瘤佔22.72%。結論在絕經後早期定...
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婦科急症385例臨牀分析
我們自2000年4月30日~2004年4月30日共行婦科急症手術385例。佔同期婦科手術的16.3%,現就其診斷和鑑別診斷做回顧性總結如下。 1臨牀資料1.1一般資料自2000年4月30日~2004年4月30日共行婦科急症手術385例,發病年齡13~58歲,平...
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血尿酸濃度與胰島素抵抗的相關性研究(對385例高尿酸血癥患者的臨牀統計分析)
...討高尿酸血癥與胰島素抵抗的相關性。方法觀察並統計了385例高尿酸血癥患者的高血壓(HBP)、糖尿病/IGT(DM/IGT)、冠心病(CHD)、腦血管意外(Stroke)的發病情況,同時檢測了他們的血尿酸濃度(UA)、血漿甘油三酯(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次香山科學會議聚焦自組裝本質規律研究
...“功能超分子體系:多層次的分子組裝體爲主題的第385次香山科學會議的中外專家指出,揭示自組裝的本質和規律是當前自組裝研究的迫切需求;儘管國內外自組裝的研究取得了較快發展,但依然有許多問題亟待研究。構建...
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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...