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氯氮平-N-氧化物 |
| CAS No.: |
34233-69-7 |
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中文名称氯氮平-N-氧化物中文同义词氯氮平氮氧化合物;氯氮平N-氧化物;氯氮平氮氧化物;氯氮平EP杂质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)英文名称CLOZAPINEN-OXIDE英文同义词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号34233-69-7分子式C18H19ClN4O分子量342.82EINECS号相关类别抑制剂;杂质对照品;VariousMetabolitesandImpurities;MetabolitesMol文件34233-69-7.mol结构式氯氮平-N-氧化物性质熔点190-248°C闪点9℃储存条件-20°CFreezer,UnderInertAtmosphere溶解度溶于二甲基亚砜。酸度系数(pKa)6.86±0.20(Predicted)形态粉末颜色粘黄色稳定性自购买之日起，稳定期为1年。其DMSO或乙醇溶液可在-20°C下保存长达3个月。InChIKeyOGUCZBIQSYYWEF-UHFFFAOYSA-N氯氮平-N-氧化物Chemicalbook用途与合成方法生物活性ClozapineN-oxide(CNO)是一种Clozapine(GLXC-06516)的代谢产物，是humanmuscarinicdesignerreceptors(DesignerReceptorsExclusivelyActivatedbyDesignerDrugs,DREADDs)的激动剂。Clozapine是一种有效的dopamine(DA)拮抗剂和选择性的muscarinicM4receptor的激动剂。靶点TargetValueDREADD()Dopaminereceptor()muscarinicM4receptor()体外研究ClozapineN-oxide(CNO)canbindtonon-DREADDreceptorsatconcentrationsrequiredforDREADDactivation,andundergoesreverse-metabolismtoitsparentcompoundclozapine,anatypicalantipsychoticthatactsatavarietyofpharmacologicaltargetsandproducesnumerousphysiologicalandbehavioraleffects.体内研究Afterasingleintraperitoneal(i.p.)injectionofClozapineN-oxide(1mg/kg)intomice,ClozapineN-oxide(CNO)plasmalevelspeakat15minandareverylowafter2h.Despitetheshortplasmahalf-lifeofCNOinmice,thebiologicaleffectsthathavebeendescribedafteracutetreatmentofDREADD-expressingexperimentalanimalsareusuallymuchlonger(6-10h). |
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