l-Pindolol-minus-Pindolol-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEl-PindololCat.No.:HY-100606CASNo.:26328-11-0Synonyms:(-)-Pindolol;(S)-(-)-Pindolol;S-Pindolol分⼦式:C₁₄H₂₀N₂O₂分⼦量:248.32作⽤靶点:5-HTReceptor;AdrenergicReceptor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:100mg/mL(402.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.0271mL20.1353mL40.2706mL5mM0.8054mL4.0271mL8.0541mL10mM0.4027mL2.0135mL4.0271mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(10.07mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(10.07mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性l-Pindolol((-)-pindolol)⼀种可逆的，竞争性的，有⼝服活性的5-HT1A/1B拮抗剂。l-Pindololβ-adrenoceptor的部分激动剂。l-Pindolol可⽤于神经系统疾病的研究。体外研究l-Pindolol(500nMand1μM)antagonizesthehyperpolarizingeffectofboth5-carboxamidotryptamine(5-CT;10nM)and5-Hydroxytryptamine(5-HT;15μM)bytestingthemembranehyperpolarizationinducedby5-CTor5-HTonCA1pyramidalcells[1].l-Pindolol(1nM-100μM)inhibitsthehyperpolarizationinthehippocampusofCA1pyramidalcellsthatinducedby100nM5-CTwithanIC50valueof92nM[1].l-Pindolol(1nM-100μM)inhibitsthehyperpolarizationofCA3neuronesinducedby300nM5-CTwithanIC50valueof522nM[1].体内研究l-Pindolol(15mg/kg;i.p.,pretreatmentbefore[3H]-WAY100635injection)reduces[3H]-WAY100635accumulationof5-HT1Areceptor-containingbrainareas[1].AnimalModel:MaleSpragueDawleyrats[1]Dosage:15mg/kgAdministration:Intraperitonealinjection;15mg/kg,20minacutetreatmentor24h,16hand20minshort-termtreatmentbefore[3H]-WAY100635injectionResult:Reduced[3H]-WAY100635accumulationin5-HT1Areceptor-containingbrainareas,butshowednoeffectonthedorsalraphenucleus(DRN),andtheCA1andCA3hippocampalareas.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forrese