SB-200646A-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESB-200646ACat.No.:HY-103129CASNo.:143797-62-0分⼦式:C₁₅H₁₅ClN₄O分⼦量:302.76作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(825.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3029mL16.5147mL33.0295mL5mM0.6606mL3.3029mL6.6059mL10mM0.3303mL1.6515mL3.3029mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性SB-200646A第⼀个对5-HT2B/2C的选择性超过5-HT2A的拮抗剂，5-HT2B，5-HT2C和5-HT2A的pKi值分别为7.5、6.9和5.2。SB-200646A具有⼝服活性，在体内具有电⽣理和抗焦虑特性。IC50&Target5-HT2BReceptor5-HT2CReceptor5-HT2AReceptor7.5(pKi)6.9(pKi)5.2(pKi)体外研究SB200646A(4μM)abolishestheethanol-inducedincreaseinminiatureinhibitorypostsynapticcurrent1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE(mIPSC)frequencyandhadnoeffectonbasalmIPSCfrequency[1].体内研究SB-200646A(20mg/kg;intravenousinjection;daily;for21days;malealbinoSprague-Dawleyrats)treatmentsignificantlydecreasesthenumberofspontaneouslyactiveventraltegmentalarea(VTA)dopaminergicneurons[1].Thei.v.administrationof4-16mg/kgofSB-200646Asignificantlyincreasesthefiringrateand%eventsasburstsinspontaneouslyactiveVTAdopaminergicneuronsandsignificantlyincreasesthe%eventsasburstinsubstantianigraparscompacta(SNC)dopaminergicneurons[1].AnimalModel:MalealbinoSprague-Dawleyrats(200-225gatthebeginningoftreatmentand300-350gatthetimeoftheexperiment)[1]Dosage:20mg/kgAdministration:Intravenousinjection;daily;for21daysResult:Significantlydecreasedthenumberofspontaneouslyactiveventraltegmentalarea(VTA)dopaminergicneurons.REFERENCES[1].BlackburnTP,etal.Theacuteandchronicadministrationofthe5-HT(2B/2C)receptorantagonistSB-200646Asignificantlyalterstheactivityofspontaneouslyactivemidbraindopamineneuronsintherat:Aninvivoextracellularsinglecellstudy.Synapse.2006Jun15;59(8):502-12.[2].KennettGA,etal.InvivopropertiesofSB200646A,a5-HT2C/2Breceptorantagonist.BrJPharmacol.1994Mar;111(3):797-802.[3].TheileJW,etal.Roleof5-hydroxytryptamine2CreceptorsinCa2+-dependentethanolpotentiationofGABAreleaseontoventraltegmentalareadopamineneurons.JPharmacolExpTher.2009May;329(2):625-33.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F