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氯氮平-N-氧化物 |
| CAS No.: |
34233-69-7 |
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中文名稱氯氮平-N-氧化物中文同義詞氯氮平氮氧化合物;氯氮平N-氧化物;氯氮平氮氧化物;氯氮平EP雜質(zhì)8;氯氮平N-氧化;8-氯-4-甲基-5H-二苯并[B,E][1,4]二氮哌嗪;氯氮平N-OXIDE;CLOZAPINEN-OXIDE(4-OXIDO-PIPRAZINYL)英文名稱CLOZAPINEN-OXIDE英文同義詞e)(1,4)diazepine,8-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(n-oxide;CLOZAPINEN-OXIDE;8-CHLORO-11-[4-METHYL-1-PIPERAZINYL]-5H-DIBENZO[B,E][1,4]DIAZEPINEN-OXIDE;MAJORMETABOLITEOFCLOZAPINE.POSSESSESLITTLEORNOACTIVITYAT5-HTRECEPTORS;ClozapineN-oxideMethanolAdduct;ClozapineN-oxidesolution;ClozapineN-oxide(CNO);8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepineCAS號34233-69-7分子式C18H19ClN4O分子量342.82EINECS號相關類別抑制劑;雜質(zhì)對照品;VariousMetabolitesandImpurities;MetabolitesMol文件34233-69-7.mol結構式氯氮平-N-氧化物性質(zhì)熔點190-248°C閃點9℃儲存條件-20°CFreezer,UnderInertAtmosphere溶解度溶于二甲基亞砜。酸度系數(shù)(pKa)6.86±0.20(Predicted)形態(tài)粉末顏色粘黃色穩(wěn)定性自購買之日起，穩(wěn)定期為1年。其DMSO或乙醇溶液可在-20°C下保存長達3個月。InChIKeyOGUCZBIQSYYWEF-UHFFFAOYSA-N氯氮平-N-氧化物Chemicalbook用途與合成方法生物活性ClozapineN-oxide(CNO)是一種Clozapine(GLXC-06516)的代謝產(chǎn)物，是humanmuscarinicdesignerreceptors(DesignerReceptorsExclusivelyActivatedbyDesignerDrugs,DREADDs)的激動劑。Clozapine是一種有效的dopamine(DA)拮抗劑和選擇性的muscarinicM4receptor的激動劑。靶點TargetValueDREADD()Dopaminereceptor()muscarinicM4receptor()體外研究ClozapineN-oxide(CNO)canbindtonon-DREADDreceptorsatconcentrationsrequiredforDREADDactivation,andundergoesreverse-metabolismtoitsparentcompoundclozapine,anatypicalantipsychoticthatactsatavarietyofpharmacologicaltargetsandproducesnumerousphysiologicalandbehavioraleffects.體內(nèi)研究Afterasingleintraperitoneal(i.p.)injectionofClozapineN-oxide(1mg/kg)intomice,ClozapineN-oxide(CNO)plasmalevelspeakat15minandareverylowafter2h.Despitetheshortplasmahalf-lifeofCNOinmice,thebiologicaleffectsthathavebeendescribedafteracutetreatmentofDREADD-expressingexperimentalanimalsareusuallymuchlonger(6-10h). |
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