AVE0991isanonpeptideandorallyactiveAng-(1-7)agonist.AVE0991competesforhigh-affinitybindingof[¹²⁵I]-Ang-(1-7)tobovineaorticendothelialcellmembraneswithIC₅₀of21±35nM.

IC50:21±35nM(Ang-(1-7)receptor)^[1]

AVE0991isanonpeptidecompoundthatevokeseffectssimilartoAng-(1-7)ontheendothelium.AVE0991andunlabeledAng-(1-7)competeforhigh-affinitybindingof[¹²⁵I]-Ang-(1-7)tobovineaorticendothelialcellmembraneswithIC₅₀sof21±35and220±280nM,respectively.PeakconcentrationsofNOandO₂^-releasebyAVE0991sodiumsaltandAng-(1-7)(both10μM)arenotsignificantlydifferent(NO:295±20and270±25nM;O₂^-:18±2and20±4nM).However,thereleasedamountofbioactiveNOis≈5timeshigherforAVE0991incomparisontoAng-(1-7)^[1].

AVE0991(0.58nmol/g)producesasignificantdecreaseofwaterdiuresisinWTmicecomparedwithvehicle-treatedanimals(0.06±0.03mLversus0.27±0.05;n=9foreachgroup;P<0.01). the="" antidiuretic="" effect="" of="" ave="" 0991="" (ave)="" is="" associated="" with="" an="" increase="" in="" urine="" osmolality="" (1669±231.0="">₂Oversus681.1±165.8mOsm/KgH₂Oinvehicle-treatedmice;P<0.01). the="" genetic="" deletion="" of="">MasabolishestheantidiureticeffectofAVE0991duringwaterloADIng(0.37±0.10mL[n=9]versus0.27±0.03mL[n=11]inAVE0991-treatedmice).AsobservedwithC57BL/6mice,administrationofAVE0991(0.58nmol/g)inwater-loadedSwissmicealsoproducesasignificantdecreaseoftheurinaryvolumecomparedwithvehicle-treatedanimals(0.13±0.05mL[n=16]versus0.51±0.04mL[n=40];P<>^[2].OneweekoftreatmentwithAVE-0991producesasignificantdecreaseinperfusionpressure(56.55±0.86vs.68.73±0.69mmHginvehicle-treatedrats)andanincreaseinsystolictension(11.40±0.05vs.9.84±0.15ginvehicle-treatedrats),rateoftensionrise(+dT/dt;184.30±0.50vs.155.20±1.97g/sinvehicle-treatedrats),rateoftensionfall(−dT/dt;179.60±1.39vs.150.80±2.42g/sinvehicle-treatedrats).Aslightincreaseinheartrate(HR)isalsoobserved(220.40±0.71vs.214.20±0.74beats/mininvehicle-treatedrats^[3].

• [1].WiemerG,etal.AVE0991,anonpeptidemimicoftheeffectsofangiotensin-(1-7)ontheendothelium.Hypertension.2002Dec;40(6):847-52.

  [2].PinheiroSV,etal.NonpeptideAVE0991isanangiotensin-(1-7)receptorMasagonistinthemousekidney.Hypertension.2004Oct;44(4):490-6.

  [3].FerreiraAJ,etal.Thenonpeptideangiotensin-(1-7)receptorMasagonistAVE-0991attenuatesheartfailureinducedbymyocardialinfarction.AmJPhysiolHeartCircPhysiol.2007Feb;292(2):H1113-9.

Bindingof[¹²⁵I]-Ang-(1-7)isperformed.Briefly,100μgofmembranesfromprimaryculturedbovineaorticendothelialcells(BAECs,passage1)areincubatedinatotalvolumeof200μLfor45minutesat25°CinHEPES-bufferedsaline(10mMHEPES,0.1MNaCl,5mMMgCl₂)containing0.2%BSAandproteaseinhibitorcocktailComplete(BoehringerMannheim).Saturablebindingof[¹²⁵I]-Ang-(1-7)iscalculatedbysubtractingnonspecificbinding(40%to50%),determinedinthepresenceof10μMunlabeledAng-(1-7)fromtotalbinding.CompetitionexperimentswithincreasingconcentrationsofAVE0991andunlabeledAng-(1-7)areperformedinthepresenceof10nM[¹²⁵I]-Ang-(1-7).Assaysareterminatedbyvacuumfiltration(≤15mmHg)overDuraporefilters(0.65μm,Opak96-wellplates)presoakedwith1%BSA.Thefiltersarewashed3timeswitheach100μLofPBS(50mM,NaHPO₄and0.15MNaCl,pH7.2).Radioactivityondriedfiltersisquantifiedwithagammacounter^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Monkeykidney(COS)cellsandChinesehamsterovary(CHO)cellsarestablytransfectedwithrat Mas CDNAdrivenbyacytomegaloviruspromoterandselectedbyneomycin.¹²⁵I-Ang-(1-7)(0.5×10^-9 mol/L)isincubatedin24-wellplatesfor60minutesat4°Cin0.3mLofserum-freemedium(DMEM)supplementedwith0.2%BSA,0.005%bacitracin,0.1mol/LPMSF,and0.5mol/Lorthophenanthrolinewith Mas-transfectedCOScellsinthepresenceorabsenceofAVE0991(AVE,10^-10 to^-5 mol/L).After2isheswithice-coldserum-freeDMEM,cellsaredisruptedwith0.1%TritonX-100.Boundradioactivityismeasuredinagammacounter.Bindingofrhodamine-Ang-(1-7)in Mas-transfectedCHOcellsisperformedundersimilarconditionsusing2×10^-9 mol/Lrhodamine-labeled-Ang-(1-7)inthepresenceorabsenceofAVE(10^-6 mol/L),CV11974(10^-6 mol/L),orPD123319(10^-6 mol/L).NSBisdeterminedinthepresenceof10^-6mol/LAng-(1-7)^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AVE0991(AVE)ispreparedin10μMKOH(Mice)^[2].
AVE0991ispreparedin0.9%NaCl(Rat)^[3].

Mice^[2]
Swissmalemice,Mas-KO(Mas^-/-)malemiceonthepuregeneticbackgroundC57BL/6,andWTC57BL/6controlmice(Mas^+/+)areused.Waterdiuresisisinducedbyintraperitonealwaterinjection(0.05mL/gofbodyweight[BW])inconsciousmice.Drugsareadministeredinthesameinjectionwithwaterloadatprefixedvolumes(0.01mL/gBW).Inthefirstsetofexperiments,WTmice(C57BL/6,controlgroup)orMas-KOmicearetreatedwith:(1)0.58nmol/gAVE0991(n=9,control;n=11,Mas-KOmice);or(2)vehicleforAVE0991(10μMKOH,0.01mL/g;n=9,control;n=9,Mas-KO).Inthesecondset,Swissmicearetreatedwith:(1)vehicle(n=36);(2)0.58nmol/gAVE0991(n=16);(3)46pmol/gAng-(1-7)antagonistA-779(n=4);(4)2nmol/glosartanorvalsartan(n=5);(5)2nmol/gAT₂receptorantagonistsPD123319orPD123177(n=9);(6)AVE0991combinedwithA-779;(7)AVE0991combinedwithlosartanorvalsartan(n=4foreach);(8)orAVE0991combinedwithPD123319(n=5)orPD123177(n=4).Theurinaryvolumeismeasuredfor60minutesafterwaterloading,andurinesamplesareobtainedtodeterminetheosmolality.ThedoseofAVE0991isbasedinpreliminaryexperimentsperformedinSwissmice.
Rat^[3]
MaleWistarratsweighting250-300gareused.RatsaretreatedeitherwithAVE-0991(1mg/kg,n=9)orvehicle(0.9%NaCl,n=11)administeredorallybygavage.Attheendofthe7dayperiodofAVE-0991treatment,theanimalsaredecapitated10-15minafterintraperitonealinjectionof400IUofheparin.Afterthethoraxisopened,theheartiscarefullydissected,removedfromthethoraciccavity,andplacedinaplatecontainingice-coldKrebs-Ringersolution(KRS)toattenuateanypotentialcardiacdamageduringdissectionofaortaartery.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].WiemerG,etal.AVE0991,anonpeptidemimicoftheeffectsofangiotensin-(1-7)ontheendothelium.Hypertension.2002Dec;40(6):847-52.

  [2].PinheiroSV,etal.NonpeptideAVE0991isanangiotensin-(1-7)receptorMasagonistinthemousekidney.Hypertension.2004Oct;44(4):490-6.

  [3].FerreiraAJ,etal.Thenonpeptideangiotensin-(1-7)receptorMasagonistAVE-0991attenuatesheartfailureinducedbymyocardialinfarction.AmJPhysiolHeartCircPhysiol.2007Feb;292(2):H1113-9.

580.72

C₂₉H₃₂N₄O₅S₂

304462-19-9

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO

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

Purity:99.16%

SelectBatch:HY-15778-10383

DataSheet(138KB)SDS(120KB)

COA(97KB)HNMR(162KB)LCMS(193KB)

HandlingInstructions(1252KB)

• [1].WiemerG,etal.AVE0991,anonpeptidemimicoftheeffectsofangiotensin-(1-7)ontheendothelium.Hypertension.2002Dec;40(6):847-52.

  [2].PinheiroSV,etal.NonpeptideAVE0991isanangiotensin-(1-7)receptorMasagonistinthemousekidney.Hypertension.2004Oct;44(4):490-6.

  [3].FerreiraAJ,etal.Thenonpeptideangiotensin-(1-7)receptorMasagonistAVE-0991attenuatesheartfailureinducedbymyocardialinfarction.AmJPhysiolHeartCircPhysiol.2007Feb;292(2):H1113-9.

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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

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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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