WIN55,212-2(Mesylate)isapotentaminoalkylindolecannabinoid(CB)receptoragonistwithK_isof62.3and3.3nMforhumanrecombinantCB1andCB2receptors,respectively.

Ki:62.3nM(humanrecombinantCB1),3.3nM(humanrecombinantCB2)

WIN55,212-2ismorepotentinCHO-CB2cellsthaninCHO-CB1cellsbyafactorof6O.WIN55,212-2hasnoeffectonarachidonicacidreleaseinCHO-CB2orcontrolCHOcells.WIN55,212-2failstostimulateanyincreaseinintracellularCa²⁺upto10μM^[1].Inprimaryculturesofratcerebralcortexneurons,WIN55,212-2(0.01--100nM)increasesextracellularglutamatelevels,displayingabell-shapedconcentration-responsecurve.ThefacilitatoryeffectofWIN55,212-2(1nM)isfullycounteractedbySR141716A(10nM),bythereplacementofthenormalKrebsRinger-bicarbonatebufferwithalowCa²⁺medium(0.2mM)andbytheIP(3)receptorantagonistxestosponginC(1μM)^[2].WIN55,212-2evokesCGRPreleasefromTGneuronsinvitro(EC₅₀=26μM)inaconcentration-andcalcium-dependentmanner.WIN55,212-2-2neitherinhibitscapsaicin-evokesCGRPreleasenordoesitinhibitforskolin-,isoproteranol-orprostaglandinE2-stimulatedcAMPaccumulation.WIN55,212-2significantlyinhibits(EC₅₀=1.7μM)50mmK⁺-evokedCGRPreleasebyapproximately70%.WIN55,212-2inhibitionof50mmK⁺-evokedCGRPreleaseisnotreversedbyantagonistsofcannabinoidtype1(CB1)receptor,butismimicksinmagnitudeandpotency(EC₅₀=2.7μM)byitscannabinoid-inactiveenantiomerWIN55,212-2-3^[3].

IntheprefrontalcortexWIN55,212-2(0.1and1mg/kgi.p.)increasesdialysateglutamatelevelsfromoftheawakerat,whilethelower(0.01mg/kg)andthehigher(2mg/kg)dosesareineffective.FurThermore,theWIN55,212-2(0.1mg/kg)-inducedincreaseofdialysateglutamatelevelsiscounteractedbypretreatmentwiththeselectiveCB(1)receptorantagonistSR141716A(0.1mg/kg,i.p.)andbythelocalperfusionwithalow-calciumRingersolution(Ca²⁺0.2mM)^[2].WIN55,212-2(0.5,1,3,5,10and15mg/kg,i.p.)doesnotaltertheseizurethresholdatlowdoses,whilehigherdosesofthedrugsignificantlyincreasesthethresholdinadose-dependentmanner.TheanticonvulsanteffectofWIN55,212-2,whichisobservedwithdosesashighas5mg/kg,canbeobservedwithdosesaslowas0.5mg/kgingroupspre-treatedwith20mg/kgofpioglitazone^[4].

• [1].FelderCC,etal.ComparisonofthepharmacologyandsignaltransductionofthehumancannabinoidCB1andCB2receptors.MolPharmacol.1995Sep;48(3):443-50.

  [2].FerraroL,etal.ThecannabinoidreceptoragonistWIN55,212-2regulatesglutamatetransmissioninratcerebralcortex:aninvivoandinvitrostudy.CerebCortex.2001Aug;11(8):728-33.

  [3].PriceTJ,etal.Cannabinoidreceptor-independentactionsoftheaminoalkylindoleWIN55,212-2ontrigeminalsensoryneurons.BrJPharmacol.2004May;142(2):257-66.

  [4].PayandemehrB,etal.InvolvementofPPARreceptorsintheanticonvulsanteffectsofacannabinoidagonist,WIN55,212-2.ProgNeuropsychopharmacolBiolPsychiatry.2015Mar3;57:140-5.

WIN55,212-2isformulatedin1%aqueoussolutionofDMSO.

Inexperiment1,differentdosesofWIN55,212-2(0.5,1,3,5,10and15mg/kg)areinjected60minpriortothedeterminationofclonicseizurethresholdinducedbyintravenousadministrationofPTZsolution.Controlanimalsreceivethesamevolumeofthevehicle(1%aqueoussolutionofDMSO).Thedosesandtimepointarechosenonthebasisofpilotstudies.Inexperiment2,inordertoconfirmtheanticonvulsanteffectsofpioglitazone,differentdoses(10,20,40and80mg/kg)areadministered4hpriortoPTZindistinctgroupsofmice.Thecorrespondingcontrolgroupreceivetheappropriatevehicle(CMC1%)atthesametimepoint.Inexperiment3,TheadditiveantiepilepticeffectsofWIN55,212-2andpioglitazoneareexamined;micereceiveacuteadministrationofpioglitazone(10or20mg/kg)3hbeforeWIN55,212-2(0.5or1mg/kg)and4hbeforePTZ.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].FelderCC,etal.ComparisonofthepharmacologyandsignaltransductionofthehumancannabinoidCB1andCB2receptors.MolPharmacol.1995Sep;48(3):443-50.

  [2].FerraroL,etal.ThecannabinoidreceptoragonistWIN55,212-2regulatesglutamatetransmissioninratcerebralcortex:aninvivoandinvitrostudy.CerebCortex.2001Aug;11(8):728-33.

  [3].PriceTJ,etal.Cannabinoidreceptor-independentactionsoftheaminoalkylindoleWIN55,212-2ontrigeminalsensoryneurons.BrJPharmacol.2004May;142(2):257-66.

  [4].PayandemehrB,etal.InvolvementofPPARreceptorsintheanticonvulsanteffectsofacannabinoidagonist,WIN55,212-2.ProgNeuropsychopharmacolBiolPsychiatry.2015Mar3;57:140-5.

522.61

C₂₈H₃₀N₂O₆S

131543-23-2

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥34mg/mL

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

Purity:98.98%

SelectBatch:HY-13291-18285HY-13291-08993

DataSheet(122KB)SDS(120KB)

COA(94KB)HNMR(222KB)LCMS(221KB)

HandlingInstructions(1252KB)

• [1].FelderCC,etal.ComparisonofthepharmacologyandsignaltransductionofthehumancannabinoidCB1andCB2receptors.MolPharmacol.1995Sep;48(3):443-50.

  [2].FerraroL,etal.ThecannabinoidreceptoragonistWIN55,212-2regulatesglutamatetransmissioninratcerebralcortex:aninvivoandinvitrostudy.CerebCortex.2001Aug;11(8):728-33.

  [3].PriceTJ,etal.Cannabinoidreceptor-independentactionsoftheaminoalkylindoleWIN55,212-2ontrigeminalsensoryneurons.BrJPharmacol.2004May;142(2):257-66.

  [4].PayandemehrB,etal.InvolvementofPPARreceptorsintheanticonvulsanteffectsofacannabinoidagonist,WIN55,212-2.ProgNeuropsychopharmacolBiolPsychiatry.2015Mar3;57:140-5.

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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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