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Clozapine N-oxide(CNO)

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Catalog No.
A3317
Clozapine代谢产物,用于化学遗传学
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 660.00
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5mg
¥ 620.00
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10mg
¥ 950.00
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25mg
¥ 2,140.00
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50mg
¥ 3,760.00
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Background

Clozapine-N-oxide (CNO) is a metabolite of clozapine, which reduces the density of 5-HT2 receptor in rat primary cortical cells. [1] Clozapine-N-oxide (CNO) also activates an evolved M3-muscarinic receptor and then can be used in chemogenetics. [2]

Clozapine is a known atypical antipsychotic medication used in the treatment of schizophrenia. The two major metabolites of clozapine are norclozapine and clozapine-N-oxide (CNO) [3]. Clozapine is also formed from its N-oxide metabolite. It means that a reversible metabolic pathway exists for clozapine and clozapine-N-oxide (CNO) [4]. In rat primary cortical cells and SHS5Y5 neuroblastoma cells, a significant decrease was found for 5-HT2 receptor density with 200 ng/ml clozapine-N-oxide (CNO) [1]. About the method of identification, reversed-phase HPLC has been reported to detect clozapine and its two major metabolites in human plasma[5].

References:
1. P. Heiser, E. Schulte, C. Hausmann, R. Becker, H. Remschmidt, J. C. Krieg and H. Vedder, Prog Neuropsychopharmacol Biol Psychiatry 2004, 28, 297-302.
2. Armbruster BN1, Li X, Pausch MH, et al. Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand. Proc Natl Acad Sci U S A. 2007 Mar 20;104(12):5163-8.
3. S. A. Volpicelli, F. Centorrino, P. R. Puopolo, J. Kando, F. R. Frankenburg, R. J. Baldessarini and J. G. Flood, Clin Chem 1993, 39, 1656-1659.
4. M. W. Jann, Y. W. Lam and W. H. Chang, Arch Int Pharmacodyn Ther 1994, 328, 243-250.
5. A. Avenoso, G. Facciola, G. M. Campo, A. Fazio and E. Spina, J Chromatogr B Biomed Sci Appl 1998, 714, 299-308.

文献引用

1. Anderson AG, Gaffy CB, et al. "Inhibition of Epstein-Barr Virus Lytic Reactivation by the Atypical Antipsychotic Drug Clozapine." Viruses. 2019 May 17;11(5). pii: E450. PMID:31108875
2. Laura A DeNardo, Cindy D Liu, et al."Temporal Evolution of Cortical Ensembles Promoting Remote Memory Retrieval." bioRxiv. 2018 April 5.

Chemical Properties

StorageStore at -20°C
M.Wt342.82
Cas No.34233-69-7
FormulaC18H19ClN4O
Solubility≥17.15 mg/mL in DMSO, <2.23 mg/mL in EtOH, ≥49 mg/mL in H2O with gentle warming
Chemical Name3-chloro-6-(4-methyl-4-oxidopiperazin-4-ium-1-yl)-5H-benzo[b][1,4]benzodiazepine
SDFDownload SDF
Canonical SMILESC[N+]1(CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl)[O-]
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

大鼠皮层细胞

溶解方法

在DMSO中的溶解度大于10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

24 h,200 ng/ml

应用

Clozapine N-oxide (CNO)是clozapine的主要代谢产物之一。在大鼠皮层细胞中,它可以显著的减少5-HT2受体的密度[1]。在大鼠脉络丛中,Clozapine N-oxide (CNO)可抑制5-HT诱导的磷酸肌醇水解[2]。

临床实验[3]:

临床样本

34-50岁的男性精神分裂症患者

剂量

早晨8点,包裹100 mg clozapine N-oxide粉末的片剂

应用

给药clozapine,12小时后clozapine N-oxide的平均血浆浓度稍微低于另一个clozapine代谢物,desmethylclozapine。给药clozapine N-oxide,12小时后clozapine血浆浓度是clozapine N-oxide的两倍。给药clozapine N-oxide后,只有一个病人血浆中可检测到desmethylclozapine。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Heiser P, Schulte E, Hausmann C, et al. Effects of clozapine and its metabolites on the 5-HT 2 receptor system in cortical and hippocampal cells in vitro[J]. Progress In Neuro-psychopharmacology and Biological Psychiatry, 2004, 28(2): 297-302.

[2]. Kuoppamki M, Syvlahti E, Hietala J. Clozapine and N-desmethylclozapine are potent 5-HT1C receptor antagonists[J]. European Journal of Pharmacology: Molecular Pharmacology, 1993, 245(2): 179-182.

[3].Chang W H, Lin S K, Lane H Y, et al. Reversible metabolism of clozapine and clozapine N-oxide in schizophrenic patients[J]. Progress in Neuro-Psychopharmacology and Biological Psychiatry, 1998, 22(5): 723-739.

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