Description | ChlorpromazineHydrochlorideisanantagonistofthedopamineD2receptors,5-HT2Areceptors,potassiumchannel,sodiumchannel,withKiof363nMand8.3nMfordopamineD2receptorandserotonin5-HT2Areceptor,respectively. |
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IC50&Target | Ki:363nM(dopamineD2receptor),8.3nM(5-HT2Areceptor)[4] |
InVitro | Chlorpromazine(3,10,20,40,and60μM)decreasesthepeakcurrentsofhNav1.7inaconcentration-dependentmanner,withIC50of25.9μMwithaHillcoefficientof2.3.Chlorpromazine(25μM)producesstronguse-dependentinhibitionofthehNav1.7current.ChlorpromazineblocksthehNav1.7channel,independentofcalmodulin[1].ChlorpromazineblocksHERGpotassiumchannelswithanIC50valueof21.6μMandaHillcoefficientof1.11.Chlorpromazine(1,10,100μM)blocksHERGpotassiumchannelsexpressedinXenopuslaevisoocytesinaconcentration-dependentmanner.ChlorpromazineblocksHERGpotassiumchannelsintheactivatedstate[5]. |
InVivo | Chlorpromazine(2mg/kg,i.p.)-inducedneurobehaviouralabnormalities(NAs)arecharacterizedbysignificantincreaseincatalepticbehaviourandloaredspontaneousactivityreactiontimeinmice[2].Chlorpromazine(1or5mg/kg,i,p.)preventsketamine(KET)fromincreasingaveragespectralpowerofdeltaandgamma-highbandsonthe5thand10thdaysoftreatmentinrats[3]. |
ClinicalTrial | ViewMoreCollapse |
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PreparingStockSolutions |
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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AnimalAdministration [2] | Chlorpromazineisformulatedinsaline. Adultmice(8-10weeksold)weighing18-25garedividedintofivegroupsofsixmicepergroup.Thetreatmentscheduleisasfollows:Group1,control(NormalSaline:NS,10mL/kgi.p.);Group2,chlorpromazine(CPZ,2mg/kgi.p.);Group3,bromocriptine(BMC,2.5mg/kgs.c.);Group4:amlodipine(AML,1mg/kgs.c.);Group5,BMC(2.5mg/kgs.c.)+AML(1mg/kg).AnimaltreatedwithBMCorAMLortheircombinationalsoreceivechlorpromazine30minlater(i.p.).Animalsaresubjectedtovarioustestsincludingmetalbartestforcatalepsyandspontaneousactivitywheelformotorassessmentandagilityandelevatedplusmaze,hole-board,Y-maze,open-fieldtestsforlocomotoryactivity,andexploratorybehaviourrespectively.Animalsareeuthanizedeighteenhourslaterbycervicaldislocation.Thebrainisdissected,rinsedinbuffer(pH7.6)andhomogenizedwithTeflonandusedforassessmentoflipidperoxidation,reducedglutathione,superoxidedismutaseandcatalase.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
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MolecularWeight | 355.33 | ||||||||||||
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Formula | C₁₇H₂₀Cl₂N₂S | ||||||||||||
CASNo. | 69-09-0 | ||||||||||||
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Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
Solvent&Solubility | DMSO:≥60mg/mL *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">1> Purity:99.85% 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
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