Cabergolineisanergotderived-dopamineD₂-likereceptoragonistthathashighaffinityforD₂,D₃,and5-HT_2Breceptors(K_i=0.7,1.5,and1.2,respectively).

Ki:0.7(DopamineD₂receptor),1.5(DopamineD₃receptor),1.2(5-HT_2Breceptor)^[1]

CabergolineactsasapotentagonistofD₂,D₃and5-HT_2Breceptors.PretreatmentwithCabergolineinhibitsH₂O₂-inducedneuronalcelldeathinadose-dependentmanner.Inthefollowingexperiments,10µMofCabergolineisusedtoinvestigateitsneuroprotectiveeffects.MAP2stainingrevealsthatCabergolinesignificantlysuppressesthelossofneuronscausedbyH₂O₂incubation.ThedetectionofapoptoticnuclearcondensationsuggestedthatCabergolinepreventsapoptoticcelldeathfollowingH₂O₂exposure^[1].

Cabergolinehasalongereliminationhalf-life(63to109h)comparedwithotherD₂-likereceptoragonists,bothalong-lastingclinicaleffectfollowingsingle-doseadministration,andanimprovementinthequalityoflifeofpatientswithchronicdiseasesareexpected^[1].Themostsignificantreductioninrapideyemovement(REM)sleepboutnumberoccurredduringthelightphase,inwhichCabergoline-injectedfemalehandledmicehas67.3%lessREMsleepbouts(F_(1,11)=12.892,P=0.004)thanCabergoline-injectedfemalesthatarerestrained,althoughthegreatestnumberinreductionofREMsleepboutsoccurrduringthedarkphase(82.3%fewerREMsleepbouts;F_(1,11)=3.667,P=0.082).Inmalemice,CabergolinereducesbaselineProlactin(PRL)levels(98.5%;F_(1,6)=13.192,P=0.011)from5.8±1.3to0.08ng/mLwithin2hoursofinjection.Aftera7-dayrecoveryperiod,PRLlevelsreturntovaluesthatarenotdifferentfrombaseline(5.0±0.60ng/mL;F_(1,6)=0.715,P=0.43)^[2].

• [1].OdakaH,etal.Cabergoline,dopamineD2receptoragonist,preventsneuronalcelldeathunderoxidativestressviareducingexcitotoxicity.PLoSOne.2014Jun10;9(6):e99271.

  [2].JeffersonF,etal.Adopaminereceptord2-typeagonistattenuatestheABIlityofstresstoaltersleepinmice.Endocrinology.2014Nov;155(11):4411-21.

CabergolineisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse^[1].

Primarycorticalneuronsareprepared.Cabergoline(10µM;exceptforexperimentsofdose-dependency)isappliedtocorticalcellsatDIV6-7.After24-hourCabergolinetreatment(exceptforexaminationofpretreatmenttime-dependencyofCabergoline),H₂O₂(50µM;exceptforthedose-dependencyofH₂O₂)isadded.Allinhibitorsandantagonists,includingspiperone,U0126,SB203580,SP600125,AP5,andnifedipineareapplied20minbeforeCabergolineorH₂O₂addition.L-glutamateisaddedatDIV7-8forcelldeathinduction.CellsurvivalrateismeasuredbyMTTassay.Aftertheindicatedtreatmentwithdrugsiscompleted,culturemediumisreplacedwith200µLfreshmediumcontaining40µlMTTsolution(2.5mg/mL,dilutedinPBS)andcellsareincubatedat37°Cfor1.5-2.5hours.Then,200µLlysisbuffercontainingisopropylalcoholisappliedtoeachwellandmixedbypipetting.Eachsampleismovedtoa96-wellplateanditsabsorbanceat570nmismeasuredusinganiMarkMicroplateleader.Cellsurvivalrateisquantitatedbyabsorbancemeasurement,becauseMTT(yellow)isdeoxidizedtoformazan(violet)inproportiontomitochondrialactivity^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Cabergolineisdissolvedin100%pharmasolveandthendilutedwith20%β-cyclodextrininwatertoyieldafinalconcentrationof0.15-0.5mg/mL^[2].

Mice^[2]
FemaleandmaleC57BL/6Jmiceareused.Cabergolineisdissolvedin100%pharmasolveandthendilutedwith20%β-cyclodextrininwatertoyieldafinalconcentrationof0.15-0.5mg/mLCabergoline.Micereceiveda0.3-mg/kgipinjectionofCabergolineorvehicle.Alldrugsarepreparedwithin48hoursofexperimentandstoredat4°C.Solutionsareallowedtoreachatroomtemperaturebeforeinjection.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].OdakaH,etal.Cabergoline,dopamineD2receptoragonist,preventsneuronalcelldeathunderoxidativestressviareducingexcitotoxicity.PLoSOne.2014Jun10;9(6):e99271.

  [2].JeffersonF,etal.Adopaminereceptord2-typeagonistattenuatestheabilityofstresstoaltersleepinmice.Endocrinology.2014Nov;155(11):4411-21.

451.6

C₂₆H₃₇N₅O₂

81409-90-7

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥33mg/mL

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

Purity:99.47%

SelectBatch:HY-15296-16632HY-15296-26651

DataSheet(126KB)SDS(120KB)

COA(96KB)HNMR(594KB)LCMS(146KB)

HandlingInstructions(1252KB)

• [1].OdakaH,etal.Cabergoline,dopamineD2receptoragonist,preventsneuronalcelldeathunderoxidativestressviareducingexcitotoxicity.PLoSOne.2014Jun10;9(6):e99271.

  [2].JeffersonF,etal.Adopaminereceptord2-typeagonistattenuatestheabilityofstresstoaltersleepinmice.Endocrinology.2014Nov;155(11):4411-21.

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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

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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