l-Pindolol-minus-Pindolol-DataSheet-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEl-PindololCat.No.:HY-100606CASNo.:26328-11-0Synonyms:(-)-Pindolol;(S)-(-)-Pindolol;S-Pindolol分?式:C??H??N?O?分?量:248.32作?靶點:5-HTReceptor;AdrenergicReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(402.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.0271mL20.1353mL40.2706mL5mM0.8054mL4.0271mL8.0541mL10mM0.4027mL2.0135mL4.0271mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(10.07mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(10.07mM);ClearsolutionBIOLOGICALACTIVITY?物活性l-Pindolol((-)-pindolol)?種可逆的，競爭性的，有?服活性的5-HT1A/1B拮抗劑。l-Pindololβ-adrenoceptor的部分激動劑。l-Pindolol可?于神經(jīng)系統(tǒng)疾病的研究。體外研究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].體內(nèi)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