Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesNGB2904hydrochlorideCat.No.:HY-12697ACASNo.:189061-11-8分?式:C??H??Cl?N?O分?量:530.92作?靶點(diǎn):DopamineReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性NGB2904hydrochloride?種有效，選擇性，具有?服活性和可透過(guò)?腦屏障的多巴胺D3受體的拮抗劑，Ki值為1.4nM。NGB2904hydrochloride對(duì)D3的選擇性?于D2，5-HT2，α1，D4，D1和D5受體(Ki=217，223，642，>5000，>10000和>10000nM)。NGB2904hydrochloride可拮抗Quinpirole刺激的有絲分裂。NGB2904hydrochloride還可以抑制可卡因(Cocaine)的獎(jiǎng)賞效應(yīng)(成癮)和可卡因誘導(dǎo)的覓藥?為的恢復(fù)。IC50&TargetD3Receptor1.4(Ki)體外研究NGB2904antagonizesQuinpirole(100nM)-stimulatedmitogenesis,withanIC50of5.0nM[1].體內(nèi)研究NGB2904(0.1-5mg/kg;i.p.30?minpriortotest)attenuatesCocaine'srewardingeffectsasassessedbyPRself-administration,BSR,andCocaine-triggeredreinstatementofCocaine-seekingbehaviorinrats[2].NGB2904(26μg/kg;asingles.c.)enhancesamphetamine(26mg/kg)-stimulatedlocomotioninwild-typemice[3].NGB2904(0.026μg-1mg/kg;asingles.c.oroncedailyfor7d)stimulatesspontaneouslocomotioninwild-typemice[3].AnimalModel:Na?vemaleLong-Evansrats(250-300g)[2]Dosage:0.1,1,5mg/kgAdministration:I.p.30?minpriortotestResult:Loweredthebreak-pointforCocaine(0.5?mg/kg;infusion)self-administrationunder1/2progressive-ratio(PR)reinforcement.InhibitedtheCocaine(2?mg/kg;i.p.)-enhancedelectricalbrainstimulationreward(BSR).InhibitedCocaine(10?mg/kg;i.p.)-triggeredreinstatementofextinguisheddrug-seekingbehavior.REFERENCES[1].YuanJ,et,al.NGB2904andNGB2849:twohighlyselectivedopamineD3receptorantagonists.BioorgMedChemLett.1998Oct6;8(19):2715-8.[2].XiZX,et,al.ThenoveldopamineD3receptorantagonistNGB2904inhibitscocaine'srewardingeffectsandcocaine-inducedreinstatementofdrug-seekingbehaviorinrats.Neuropsychopharmacology.2006Jul;31(7):1393-405.[3].PritchardLM,et,al.ThedopamineD3receptorantagonistNGB2904increasesspontaneousandamphetamine-stimulatedlocomotion.PharmacolBiochemBehav.2007Apr;86(4):718-26.McePdfHeightMedChemExpress(MCE)只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科