Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECYB210010Cat.No.:HY-162423CASNo.:2762568-47-6分?式:C??H??ClF?NO?S分?量:317.76作?靶點(diǎn):5-HTReceptor;AndrogenReceptor作?通路:GPCR/GProtein;NeuronalSignaling;VitaminDRelated/NuclearReceptor儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性CYB210010具有?服?物利?度且長(zhǎng)效的?素5-HT2受體激動(dòng)劑，可選擇性靶向5-HT2A和5-HT2C受體(EC50:4.1nM和7.3nM)。CYB210010可進(jìn)?中樞神經(jīng)系統(tǒng)，引起頭部抽搐反應(yīng)(HTR)，且不容易在慢性給藥過(guò)程中出現(xiàn)?為耐受性。IC50&Target5-HT1AReceptor5-HT1BReceptor5-HT6Receptor5-HT7Receptor32nM(Ki)949nM(Ki)1301nM(Ki)4918nM(Ki)5-HT2AReceptor5-HT2CReceptor5-HT2BReceptor4.1nM(EC50)7.3nM(EC50)88nM(EC50)體內(nèi)研究CYB210010hascertainoralbioavailabilityandcansmoothlyenterthecentralnervoussystem,bindto5-HT2Areceptorsinthefrontalcortex,andincreasetheexpressionofneuroplasticity-relatedgenesinthefrontalcortex[1].CYB210010(0.1-3mg/kg;sc;singledose)causesaheadtwitchresponse(HTR)inmouse,andcanbeadministeredsubchronicallyatthresholddoseswithoutdevelopingbehavioraltolerance[1].AnimalModel:MaleC57BL/6Jmice[1]Dosage:0.1,0.3,1,3,mg/kgAdministration:sc;sigledoseResult:ElicitedmaximumHTRsat-15minpostadministrationwhichterminatedafter220min1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE(significantfromvehiclefrom5-160min).REFERENCES[1].VartyGB,etal.SynthesisandStructure-ActivityRelationshipsof2,5-Dimethoxy-4-SubstitutedPhenethylaminesandtheDiscoveryofCYB210010:APotent,OrallyBioavailableandLong-ActingSerotonin5-HT2ReceptorAgonist.JMedChem.2024Apr25;67(8):6144-6188.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;0