Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemESR57227ACat.No.:HY-102064CASNo.:77145-61-0分?式:C??H??Cl?N?分?量:248.15作?靶點(diǎn):5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:8.33mg/mL(33.57mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM4.0298mL20.1491mL40.2982mL5mM0.8060mL4.0298mL8.0596mL10mM0.4030mL2.0149mL4.0298mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請(qǐng)先配制澄的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(8.38mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(8.38mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(8.38mM);Clearsolution1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性SR57227A具有?服活性的5-HT3受體的?種選擇性激動(dòng)劑,可透過(guò)?腦屏障。SR57227A對(duì)???質(zhì)膜和整個(gè)NG108-15細(xì)胞或其膜上5-HT3受體結(jié)合位點(diǎn)的親和?(IC50)在2.8~250nM。具有抗抑郁作?。體外研究SR57227Abindsto5-HT3receptorslabelledwith[3H]S-zacopridewithanaffinity(Ki)of115nMinratcerebralcortex,150nMinNG108-15cellmembranesand103nMinwholeNG108-15cell[1].體內(nèi)研究SR57227A(1-30mg/kg;i.p.)dose-dependentlyreducesimmobilitytimeintheforcedswimmingtestwithanED50valueforthiseffectof14.2mg/kg[2].Intheforcedswimmingtest,SR57227Adose-dependentlyreducesthedurationofimmobilityinratsafteri.p.administration.(ED50=7.6mg/kgi.p.inrats.)SR57227Aisalsoactiveinbothspeciesafteroraladministration.Inatime-coursestudyinmice,SR57227A(20mg/kgp.o.)producesasignificanteffectlasting6hours.SR57227A(1and3mg/kgi.p.)reducestheelevationoftheescapefailuresinthelearnedhelplessnessmodelinratsby50-60%onthelasttwodaysoftheavoidancetask,andreducesisolation-inducedaggressivityinmiceby50to85%,aneffectwhichisantagonisedbyZacopride(1mg/kgi.p.)[2].REFERENCES[1].PonceletM,etal,LeFurG.Antidepressant-likeeffectsofSR57227A,a5-HT3receptoragonist,inrodents.JNeuralTransmGenSect.1995;102(2):83‐90.[2].BachyA,etal.SR57227A:apotentandselectiveagonistatcentralandperipheral5-HT3receptorsinvitroandinvivo.EurJPharmacol.1993;237(2-3):299‐309.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio