AprepitantisaspecificNK-1Rantagonist,usedasanantiemeticagent.

AprepitantdecreasesthemetabolicactivitywithanestimatedIC₅₀valueof20µM.Aprepitantinducescell-growthinhibitionandG1cell-cyclearrest.AprepitantsignificantlyinducesapoptosisinNalm-6cells,andtheapoptosisismediatedthroughcaspase-3activation.Aprepitant(20µM)inducesp53accumulationandexpressionofpro-apoptoticp53targetgenes^[2].Aprepitant(1,5,10µM)inhibitsHIVinfectioninMDMfrombothdepressedandnotdepressedHIVnegativeindividualsexvivoinadose-dependentmanner.IC₉₀valueofaprepitantisequivalentto10μM,andtheIC₅₀valueisabout5μM^[4].

AprepitantpreventstheincreaseofNK-1RexpressioninducedbyinvivoNHPinfectionwithB.burgdorferi.AprepitanttreatmentpreventsB.burgdorferi-inducedincreasesinCCL2proteinlevelsintheCSFofNHPs.AprepitanttreatmentpreventsB.burgdorferi-inducedincreasesinCCL2andCXCL13mRNAexpressioninthedorsalrootgangliaofNHPs,preventsB.burgdorferi-inducedincreasesinCCL2,CXCL13,IL-17A,andIL-6mRNAexpressioninthespinalcordofNHPs.AprepitanttreatmentattenuatesB.burgdorferiinfection-inducedreductionsinastrocyteactivity/numbers^[1].Aprepitant(10mg/kg,i.p.)significantlyattenuatestheCPPexpressionandlocomotoractivationproducedbyAMPHandcocaineinmice.Incontrast,aprepitantsignificantlyenhancestheexpressionofCPPproducedbymorphinewhilesignificantlysuppressingthelocomotoractivityofthemiceconditionedwithmorphine.AprepitantdoesnotinducesignificantCPPorconditionedplaceaversionorlocomotoractivationorsuppression^[3].Aprepitant(125mg/day,p.o.)resultsin1logreductioninplasmalevelsofviralRNAascomparedtonon-treatedcontrols^[4].

• [1].MartinezAN,etal.AprepitantlimitsinvivoneuroinflammatoryresponsesinarhesusmodelofLymeneuroborreliosis.JNeuroinflammation.2017Feb15;14(1):37.

  [2].BayatiS,etal.InhibitionoftachykininNK1receptorusingaprepitantinducesapoptoticcelldeathandG1arrestthroughAkt/p53axisinpre-Bacutelymphoblasticleukemiacells.EurJPharmacol.2016Nov15;791:274-283.

  [3].MannangattiP,etal.Differentialeffectsofaprepitant,aclinicallyusedneurokinin-1receptorantagonistontheexpressionofconditionedpsychostimulantversusopioidreward.Psychopharmacology(Berl).2017Feb;234(4):695-705.

  [4].BarrettJS,etal.PharmacologicrationalefortheNK1Rantagonist,aprepitantasadjunctivetherapyinHIV.JTranslMed.2016May26;14(1):148.

AprepitantisdissolvedinDMSO.

TheinhibitoryeffectofaprepitantonmetabolicactivityofNalm-6cellsisassessedbyuptakeofthiazolylbluetetrazoliumbromide(MTT)byviablecells.Cellsareplatedonto96-wellplatesatadensityof5000cells/well.Aftertreatmentwithaprepitantat5,10,15,20and30µMfor24,36and48h,thecellsarefurtherincubatedwith100μLofMTT(0.5mg/mL)at37°Cfor3h.Untreatedcellsaredefinedasthecontrolgroup.Followingsolubilizationofprecipitatedformazanwith100μLofDMSO,theopticaldensitometryismeasuredwithanELISAreaderatawavelengthof578nm.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Fifteenrhesusmacaquesareanesthetizedandinoculatedintrathecallywith1×10⁸livespiRochetesintothecisternamagna,whereasfiverhesusmacaquesareleftuninfectedandreceive1mLofRPMI1640mediumafterremovinganequivalentvolumeofCSF.TheestablishmentofinvivoB.burgdorferiinfectionisconfirmedbypositiveculturefromatleastnecropsytissuesample.Thefirstsetofanimalsarestudiedfor2weeksandincludedtwocontrolanimals(oneofwhichistreatedwithaprepitant),twoinfectedanduntreatedanimals,andtwoinfectedanimalsthataretreatedwithaprepitant.Thesecondsetofanimalsarestudiedfor4weeksandincludedthreecontrolanimals(oneofwhichistreatedwithaprepitant),fiveinfectedanduntreatedanimals,andfourinfectedanimalstreatedwithaprepitant.Animalsreceiveanaveragedoseofaprepitantof28 ± 6mg/kgperdayp.o.daily,anddrugtreatmentsarestarted2daysbeforeinoculation.ThesedosesareconsistentwithstandardveterinaryregimensforthechosendrugsinNHP,andthe4-weekdurationofthestudyprecludesthedevelopmentofneuralpathologythatoccursat8weeksfollowingB.burgdorferiinfection.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].MartinezAN,etal.AprepitantlimitsinvivoneuroinflammatoryresponsesinarhesusmodelofLymeneuroborreliosis.JNeuroinflammation.2017Feb15;14(1):37.

  [2].BayatiS,etal.InhibitionoftachykininNK1receptorusingaprepitantinducesapoptoticcelldeathandG1arrestthroughAkt/p53axisinpre-Bacutelymphoblasticleukemiacells.EurJPharmacol.2016Nov15;791:274-283.

  [3].MannangattiP,etal.Differentialeffectsofaprepitant,aclinicallyusedneurokinin-1receptorantagonistontheexpressionofconditionedpsychostimulantversusopioidreward.Psychopharmacology(Berl).2017Feb;234(4):695-705.

  [4].BarrettJS,etal.PharmacologicrationalefortheNK1Rantagonist,aprepitantasadjunctivetherapyinHIV.JTranslMed.2016May26;14(1):148.

534.43

C₂₃H₂₁F₇N₄O₃

170729-80-3

RoomtemperatureincontinentalUS;mayvaryelsewhere

10mMinDMSO

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.32%

SelectBatch:HY-10052-07960HY-10052-25547

DataSheet(134KB)SDS(120KB)

COA(95KB)LCMS(166KB)

HandlingInstructions(1252KB)

• [1].MartinezAN,etal.AprepitantlimitsinvivoneuroinflammatoryresponsesinarhesusmodelofLymeneuroborreliosis.JNeuroinflammation.2017Feb15;14(1):37.

  [2].BayatiS,etal.InhibitionoftachykininNK1receptorusingaprepitantinducesapoptoticcelldeathandG1arrestthroughAkt/p53axisinpre-Bacutelymphoblasticleukemiacells.EurJPharmacol.2016Nov15;791:274-283.

  [3].MannangattiP,etal.Differentialeffectsofaprepitant,aclinicallyusedneurokinin-1receptorantagonistontheexpressionofconditionedpsychostimulantversusopioidreward.Psychopharmacology(Berl).2017Feb;234(4):695-705.

  [4].BarrettJS,etal.PharmacologicrationalefortheNK1Rantagonist,aprepitantasadjunctivetherapyinHIV.JTranslMed.2016May26;14(1):148.

品牌介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-Tropanylindole-3-carboxylate;lαH，5Αh-Tropan-3α-ylindole-3-carboxylate中文名称:托烷司琼中文同义词:托普西隆;托普西龙;曲匹西龙;托烷司琼;Β-托烷司琼;CS-348;Β-内托烷司琼;吲哚-3-甲酰氯;Β-托烷司琼(光学异构体);Β-托烷司琼,托烷司琼异构体CBNumber:CB3236404分子式:C17H20N2O2分子量:284.35MOLFile:89565-68-4.mol化学性质安全信息用途供应商112化学性质安全信息用途供应商112托烷司琼化学性质熔点:201-202°C沸点:448.5±35.0°C(Predicted)密度:1.26储存条件:2-8°C溶解度:H2O:soluble形态:solid酸度系数(pKa):15.38±0.30(Predicted)颜色:whiteCAS数据库:Chemicalbook89565-68-4(CASDataBaseReference)安全信息WGKGermany:3托烷司琼化学药品说明书托烷司琼|药物应用信息托烷司琼性质、用途与生产工艺临床评价Sorbe等报道本品对含顺铂(剂量50～89mg/m2)化疗方案引起的急性呕吐完全控制率为63%。58例恶性肿瘤化疗所致恶心、呕吐者，应用托烷司琼或昂丹司琼8mg分别在同一病人前后2个化疗周期的第1d给药前30min静脉注射，并用地塞米松10mg静脉滴注。结果两药控制急性及迟发性恶心、呕吐的疗效基本相似，均可达81%～100%。本品对强致吐化疗药物顺铂的止吐疗效突出。药物相关作用饮食可略为延长本品的吸收。本品与利福平、苯巴比妥等肝酶诱导药同时使用，可加快代谢，故快代谢型者需增加剂量，慢者则不必。西咪替丁等肝酶抑制药对本品血药浓度无明显影响。适应症托烷司琼临床用于预防和治疗癌症化疗引起的恶心和呕吐。化学性质结晶，熔点201-202℃(二氯甲烷-乙酸乙酯)。单盐酸托烷司琼(TropisetronMonohydroehloride)：C17H20N2O2?HCI。[105826-92-4]。熔点283-285℃(分解)。用途有高效性和选择性的5-HT3受体拮抗剂。用于化疗所致的呕吐。用途为5-羟色胺拮抗药生产方法托品醇(I)和酰氯(Ⅱ)反应，可得托烷司琼。托烷司琼上下游产品信息上游原料托品醇下游产品

公司介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-

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