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ModifiedReceptorInternalizationuponCoexpressionof5-HT1BReceptorand5-HT2BReceptors
【关键词】ModifiedSerotonin5-HT2Breceptorsareoftencoexpressedwith5-HT1Breceptors,andcross-talkbetweenthetworeceptorshasbeenreportedinvariouscelltypes.However,manymechanisticdetailsunderlying5-HT1Band5-HT2Breceptorcross-talkhavenotbeenelucidated.Wehypothesizedthat5-HT2Band5-HT1Breceptorseachaffe...
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CharacterizationoftheNovelHumanSerotoninReceptorSubunits5-HT3C,5-HT3D,and5-HT3E
...acterizationWithinthefamilyofserotoninreceptors,the5-hydroxytryptamine-3(5-HT3)receptoristheonlyligand-gatedionchannel.Itiscomposedoffivesubunits,ofwhichthe5-HT3Aand5-HT3Bsubunitsarebestcharacterized.Severalstudies,however,havereportedonthefunctionaldiversityofnative5-HT3receptors,whichcannotsolelyb...
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AnandamideInhibitionof5-HT3AReceptorsVarieswithReceptorDensityandDesensitization
...GICs.Here,wereportthatAEAinhibitedthefunctionofserotoningatedionchannels(5-HT3A)expressedinXenopuslaevisoocytesandhumanembryonickidney293cellsinamannerthatwasdependentonthesteady-statereceptordensityatthecellsurface.ThemagnitudeofAEAinhibitionwasinverselycorrelatedwiththeexpressionlevelsofreceptorpr...
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SerotoninInhibitsNeuronalExcitabilitybyActivatingTwo-PoreDomainK+ChannelsintheEntorhinalCortex
...ftheECbyactivatingtheTWIK-1typeofthetwo-poredomainK+channels.Theeffectsof5-HTweremediatedvia5-HT1AreceptorsandrequiredthefunctionofGi3subunitandproteinkinaseA.Serotonin-mediatedinhibitionofECactivityresultedinaninhibitionofhippocampalfunction.Ourstudyprovidesacellularmechanismthatmightatleastpartial...
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RisperidoneIrreversiblyBindstoandInactivatestheh5-HT7SerotoninReceptor
...键词】RisperidoneRisperidonedisplaysanovelmechanismofantagonismoftheh5-HT7receptor.Pretreatmentofthecellswith5or20nMrisperidone,followedbyremovalofthedrugfromthemedia,rendersthe5-HT7receptorsunresponsiveto10µM5-HTforatleast24h.Thus,risperidoneseemstobeproducingarapid,long-lastinginactivatio...
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PharmacologicalCharacterizationofSerotonergicReceptorActivityintheHypoglossalNucleus
...essedthedose–responsecurveforthe2Cagonist.Rapiddesensitizationoccurredwiththe2Cagonistonly(p0.05).The7antagonist,SB-269,970,hadnoeffectoneitherintrinsicactivityoragonistresponses.Weconcludethatserotonin2Aisthepredominantexcitatoryserotoninreceptorsubtypeathypoglossalmotorneurons.Theserotonin2Cexci...
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DualSerotonergicRegulationofVentricularContractileForceThrough5-HT2Aand5-HT4ReceptorsInducedintheAcuteFailingHeart
...leftventriclehasbecomesensitivetoserotoninbecauseofappearanceofGs-coupled5-HT4receptors.WhetherthisalsooccursinacuteCHFisunknown.Serotoninresponsivenessmaydevelopgraduallyorrepresentanearlyresponsetotheinsult.Furthermore,serotoninreceptorexpressioncouldvarywithprogressionofthedisease.PostinfarctionC...
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MolecularDeterminantsfortheInteractionoftheValvulopathicAnorexigenNorfenfluraminewiththe5-HT2BReceptor
...e-threateningcardiovascularsideeffects.SNFreducesappetitethroughserotonin5-HT2Creceptoractivation;itcausescardiopulmonarysideeffectsthrough5-HT2Breceptoractivation.Thus,weattemptedtoidentifymoleculardeterminantsofSNFbindingto5-HT2BreceptorsdistinctfromthoseunderlyingSNF-5-HT2C/2Areceptorinteractions...
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RegionalDifferencesintheCouplingof5-Hydroxytryptamine-1AReceptorstoGProteinsintheRatBrain
...词】5-Hydroxytryptamine-1ANumerousdatashowedthat5-hydroxytryptamine-1A(5-HT1A)receptorscoupletoGo/iproteinsforsignaltransduction.However,thesubunitisoformsreallyinvolvedin5-HT1Areceptorcouplinginbrainremaintobeidentified.Moreover,regionaldifferencesinthefunctionalcharacteristicsofbrain5-HT1Arecept...
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ARoleforSerotonin(-HT)inHepaticStellateCellFunctionandLiverFibrosis
...icalandneurotrophicfactors.Thisstudyaddressesthepotentialfortheserotonin(5-HT)systemtoinfluenceHSCbiology.RatandhumanHSCsexpressthe5-HT1B,5-HT1F5-HT2A5-HT2B,and5-HT7receptors,withexpressionof5-HT1B5-HT2Aand5-HT2BbeinginducedonHSCactivation.Inductionof5-HT2Aand5-HT2Bwas106??39-and52??8.5-foldthatofqu...
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InverseAgonistandNeutralAntagonistActionsofAntidepressantsatRecombinantandNative5-Hydroxytryptamine2CReceptors:DifferentialModulationofCellS
【关键词】InverseDespitetheimportanceof5-hydroxytryptamine(5-HT)2C(serotonin)receptorsinthecontrolofdepressivestates,actionsofantidepressantsatthesereceptorsremainpoorlycharacterized.Thisissuewasaddressedbothinhumanembryonickidney(HEK)-293cellscoexpressinguneditedhuman5-HT2CINIreceptorsandGqpro...
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TheNaturalMutationEncodingaCTerminus-Truncated5-Hydroxytryptamine2BReceptorIsaGainofProliferativeFunctions
...ions,fewfunctionalmutationshavebeenidentifiedinthehuman5-hydroxytryptamine(HT)2Breceptorgene.AheterozygousmutationR393Xinthe5-HT2Breceptorwasrecentlyidentifiedinapatientdiagnosedwithpulmonaryhypertensionafterintakeoftheanorexigenicdexfenfluramine.Althoughreportedtogeneratealackoffunction,thisCtermin...
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Serotonin5-Hydroxytryptamine2CReceptorSignalinginHypothalamicProopiomelanocortinNeurons:RoleinEnergyHomeostasisinFemales
...mitterreceptorsignalingpathwaysconvergetocontrolenergyhomeostasis.Because5-HT2CreceptorsmediatemanyoftheeffectsofserotonininPOMCneurons,weelucidatedthecommonsignalingpathwaysofE2and5-HTinguineapigsusingsingle-cellreversetranscription-polymerasechainreaction(RT-PCR),realtimeRT-PCR,andwhole-cellpatchr...
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Palmitoylationofthe5-Hydroxytryptamine4aReceptorRegulatesReceptorPhosphorylation,Desensitization,and-Arrestin-MediatedEndocytosis
...,Montpellier,France(A.D.,F.G.,G.B.)AbstractThemouse5-hydroxytryptamine4a(5-HT4a)receptorisanunusualmemberoftheGprotein-coupledreceptorsuperfamilybecauseitpossessestwoseparatecarboxyl-terminalpalmitoylationsites,whichmayallowthereceptortoadoptdifferentconformationsinanagonist-dependentmanner(JBiolChe...
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5-HT1A受体的作用及其临床意义
【关键词】5-HT1A受体 5-羟色胺再摄取抑制剂(SSRI)是近十余年临床广泛应用的抗抑郁剂,有疗效好、不良反应轻和服药简便等多方面的优点,但在应用过程中也有起效较慢的缺点,特别是在抑郁症状严重需尽快解除时更显得...
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NativeRatHippocampal5-HT1AReceptorsShowConstitutiveActivity
...关键词】NativePreviousstudieshaveshownthathuman5-hydroxytryptamine(5-HT)1AreceptorsstablyexpressedintransfectedcelllinesshowconstitutiveG-proteinactivity,asrevealedbytheinhibitoryeffectofinverseagonists,suchasspiperone,onbasalguanosine-5‘-O-(3-[35S]thio)-triphosphate([35S]GTPS)binding.Inthepre...
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5-HT细胞移植对慢性不可预见性抑郁症大鼠多器官损伤的作用与可能性机制
【摘要】目的探讨外源性5-HT神经细胞移植对慢性不可预见性应激大鼠多内脏器官损伤的作用。方法将40只雄性SD大鼠(购置第二军医大学实验动物中心)随机分为4组(10只/组):正常对照组(Ⅰ)、慢性应激组(Ⅱ)、慢性应激...
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5-羟色胺与食欲抑制剂
5-羟色胺(5-hydroxytryptamine,5-HT)又称血清素(serotonin),是人体重要的活性物质,5-HT在突触间隙消除的方式是通过重摄取和酶降解两种机制,其中以重摄取为主,5-HT受体亚型非常多,并且分布极为广泛,所以,5-HT神经元无论...
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MappingResiduesintheLigand-BindingDomainofthe5-HT3Receptorontod-TubocurarineStructure
【关键词】MappingResiduesTheserotonin5-HT3receptor(5-HT3R)isamemberofthecys-loopligand-gatedionchannelfamily.Wehaveusedthecombinationofsite-directedmutagenesis,homologymodelingofthe5-HT3Rextracellulardomain,andliganddockingsimulationsasawaytomapthearchitectureofthe5-HT3Rligandbindingdomain.Muta...
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国际高血压防治指南对高血压定义、分层、诊断性评价的建议
【摘要】本文根据近年发表的国际高血压(HT)指南资料,对HT的流行病学情况,定义,血压(BP)水平分级,危险分层及诊断性评估等建议作一简要介绍【关键词】高血压定分层诊断性评估【Abstract】Thisarticlereviewsepidemiologicalstat...
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新型抗抑郁药的机制与应用的临床分析
...,发生机制及临床表现 1.1抑郁症发生与5-羟色胺(5-HT)、去甲肾上腺素(NE)和多巴胺(DA)能投射不足有关:(1)当投射到额叶皮质,表现:抑郁心境和注意迟缓;(2)当投射到边缘,表现内疚、自残、自杀;(3)当投...
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SpatialOrientationoftheAntagonistGranisetronintheLigand-BindingSiteofthe5-HT3Receptor
...egeofMedicine,Philadelphia,PennsylvaniaAbstractTheserotonintype3receptor(5-HT3R)isamemberofthecys-loopligand-gatedionchannel(LGIC)superfamily.Likealmostallmembraneproteins,high-resolutionstructuraldataareunavailableforthisclassofreceptors.WehavetakenadvantageofthehighdegreeofhomologybetweenLGICsandt...
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研究发现五羟色胺控制雌性动物性偏好
...爱等在《自然》发表文章,他们发现脑内的5-羟色胺(5-HT)控制雄鼠的性偏好行为:缺乏脑内5-HT的雄鼠丧失偏好、同等追求雌鼠和雄鼠,提示脑内神经递质5-HT是雄性哺乳动物脑中对其性偏好至关重要的分子。这一工作引出自然...
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关联5-羟色胺与食物摄入量调控的机制
...而且可能让科学家开发出副作用更少的减肥药物。包括5-HT2C受体(5-HT2CR)亚型在内的5-羟色胺(5-HT)系统已经被证明在调控能量的体内平衡方面扮演着一个重要的角色。此前的研究证明了过度食物摄入和肥胖与5-HT2CR缺乏有联系...
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丁螺环酮的精神科应用
...放激素和皮质醇水平,通过激动盐皮质激素受体而降低5-HT1A受体密度和mRNA水平,当5-HT1A受体密度降低后,γ-氨基丁酸的α1和α2受体亚单位向下调节,对应激的阈值降低,易感焦虑[1]。丁螺环酮激动海马和杏仁核突触后膜的5-HT...
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PhosphorylationofG11ProteinContributestoAgonist-InducedDesensitizationof5-HT2AReceptorSignaling
...sphorylationofGq/11proteinsinagonist-induceddesensitizationofserotonin2A(5-HT2A)receptors.Inanembryonicratcorticalcellline(A1A1v),24-htreatmentwith100nM(-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropaneHCl(DOI),a5-HT2A/2Creceptoragonist,decreasedDOI-stimulatedinositolphosphateaccumulationandincreased...
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电针对大脑中动脉缺血/再灌注模型大鼠脑内5-羟色胺含量及局部脑血流量的影响
...灌注模型,研究电头针、电体针对大鼠脑内5-羟色胺(5-HT)含量及局部脑血流量(rCBF)的影响。 1材料与方法 1.1实验动物共采用健康成年SD大鼠29只,来源于华中科技大学同济医学院实验动物中心,雌雄不拘,体重250~300...
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LocalizationoftheMouse5-Hydroxytryptamine1AReceptorinLipidMicrodomainsDependsonItsPalmitoylationandIsInvolvedinReceptor-MediatedSignaling
...edwild-typeandpalmitoylation-deficientmouse5-hydroxytryptamine1Areceptor(5-HT1A)receptorsfusedtotheyellowfluorescentprotein-andthecyanfluorescentprotein(CFP)-taggedi3subunitofheterotrimericG-proteintostudyspatiotemporaldistributionofthe5-HT1A-mediatedsignalinginlivingcells.Wealsoaddressedthequestion...
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MolecularInteractionofSerotonin5-HT2AReceptorResiduesPhe339(6.51)andPhe340(6.52)withSuperpotentN-BenzylPhenethylamineAgonists
...ductedtoexaminethemolecularbasisforthehighaffinityandpotencyofanewclassof5-HT2Areceptoragonists,N-benzylphenethylamines.CompetitionbindingassaysatseveralserotoninreceptorsconfirmedthatanN-arylmethylsubstitutionwasnecessaryforaffinityincreasesupto300-foldoversimpleN-alkylhomologs,aswellasenhancedsele...
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奥氮平与氯丙嗪对男性精神分裂症患者攻击性行为及血浆5-羟色胺的影响
...嗪对男性精神分裂症患者攻击性行为及血浆5-羟色胺(5-HT)的影响。方法以既往史和外显攻击行为量表(MOAS)评分,将有攻击行为的男性精神分裂症患者68例随机分为奥氮平组和氯丙嗪组,治疗6周。用放射免疫法测定治疗前后...