Tetrodotoxinisahighlyselectivesodiumchannelblocker,withIC₅₀of33nMforNav1.6.

Sodiumchannel^[1]
IC50:33nM(Nav1.6)^[2]

Thesodiumchannel(Nav)genefamilyisclassifiedintoTetrodotoxin-sensitive(TTX-S;Nav1.1,Nav1.2,Nav1.3,Nav1.4,Nav1.6,andNav1.7)andTTX-resistant(TTX-R)channels(Nav1.5,Nav1.8,andNav1.9),eachofwhichisassociatedwithspecifictherapeuticindicationsbasedontheirexpressionpattern,function,andgeneticmutations.Morethan97%ofmacroscopicNavcurrentinND7-23cellsiscarriedbyTetrodotoxin-sensitivechannels(300nMTTX)andthatNav1.7isthepredominantchannelcontributingtothisresponse(65%ofpeakinwardcurrent),followedbyNav1.6(~20%)andnegligIBLeNav1.3currents(~2%).Inaddition,Tetrodotoxin(TTX)isselectivefortheNav1.6(IC₅₀of33nM)and50-foldoverNav1.7inhumanNavchannelsexpressedinmammaliancells,confirmingpreviousstudiesofrodentNavchannelsexpressedinoocytesandHEKcells^[2].

• [1].NgocAH,etal.Tetrodotoxinformoderatetoseverecancerpain:arandomized,doubleblind,paralleldesignmulticenterstudy.JPainSymptomManage.2008Apr;35(4):420-9.

  [2].RogersM,etal.CharacterizationofEndogenousSodiumChannelsintheND7-23NeuroblastomaCellLine:ImplicationsforUseasaHeterologousIonChannelExpressionSystemSuitableforAutomatedPatchClampScreening.AssayDrugDevTechnol.2016Mar;14(2

Tetrodotoxin(TTX)isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse^[2].

CHOandHEKheterologouscelllinesstablyexpressinghNav1.3(CYL3003),hNav1.6(CYL3010),andhNav1.7channels(CYL3011)aregrown.CurrentsareelicitedfromNav1.3,Nav1.6,andNav1.7celllinesandND7-23cellsusingastandardtwo-pulsevoltageprotocol.Fromaholdingpotentialof−100mV,a20-msactivatingsteptothepeakoftheIVforeachNav1.xchannel(0,−10,−20,and−10mVforNav1.3,Nav1.6,Nav1.7,andTTX-S,respectively)isappliedtoassesstheeffectofcompoundsonchannelsopenedfromtheresting(closed)state(Peak1).Thesecondactivatingpulseisappliedfollowinga5-sprepulsetoamembranepotentialthatinduces~50%inactivationofavailablechannelstoassessblockontheinactivatedstateofthechannel.Thehalf-inactivatingpotentialvarieddependingonNav1.xtypeandtissuecultureconditionsandisadjustedeachdayforeachtarget(typicallyrangingbetween−70and−50mV).Thetwo-stepvoltageprotocolisappliedatasweepintervalof0.067Hzthroughoutthedurationoftheexperiment.Leaksubtractionisappliedbetweenthevoltagesweeps,butthelengthofthevoltageprotocolonlyallowedtwoleaksweepsperepoch,limitingtheirutilityandouruseofthismethod.Rather,sweepsubtractionisemployedintheQPatchsoftwarethatenablesasingleoraveragednumberofsweepstobesubtractedfromallothersweepsintheexperiment;applyingasaturatingdoseof300nMTetrodotoxin(TTX)toeachcellattheendofeveryexperimentenabledeffectivesweepsubtractionandremovalofcapacitiveartifactsandcontaminating(e.g.,outward)currents^[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].NgocAH,etal.Tetrodotoxinformoderatetoseverecancerpain:arandomized,doubleblind,paralleldesignmulticenterstudy.JPainSymptomManage.2008Apr;35(4):420-9.

  [2].RogersM,etal.CharacterizationofEndogenousSodiumChannelsintheND7-23NeuroblastomaCellLine:ImplicationsforUseasaHeterologousIonChannelExpressionSystemSuitableforAutomatedPatchClampScreening.AssayDrugDevTechnol.2016Mar;14(2

319.27

C₁₁H₁₇N₃O₈

4368-28-9

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO

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

Purity:99.99%

SelectBatch:HY-12526-24643HY-12526-22606HY-12526-21829HY-12526-18968HY-12526-26997HY-12526-20245

DataSheet(123KB)SDS(389KB)

COA(96KB)HNMR(254KB)RP-HPLC(258KB)

HandlingInstructions(1252KB)

• [1].NgocAH,etal.Tetrodotoxinformoderatetoseverecancerpain:arandomized,doubleblind,paralleldesignmulticenterstudy.JPainSymptomManage.2008Apr;35(4):420-9.

  [2].RogersM,etal.CharacterizationofEndogenousSodiumChannelsintheND7-23NeuroblastomaCellLine:ImplicationsforUseasaHeterologousIonChannelExpressionSystemSuitableforAutomatedPatchClampScreening.AssayDrugDevTechnol.2016Mar;14(2

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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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类固醇 生物碱 糖类和糖苷类 染料试剂 生化分析试剂

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