Clozapine N-oxide(CNO)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Clozapine-N-oxide（CNO）是一种Clozapine代谢产物，可以降低大鼠初级皮层细胞5-HT2受体的密度[1]。Clozapine-N-oxide (CNO)也可激活一种进化的M3-毒蕈碱受体，因而可用于chemogenetics[2]。
Clozapine是一种已知的非典型抗精神病药物，用于治疗精神分裂症。Clozapine的两中主要代谢产物为norclozapine和clozapine-N-oxide（CNO）[2]。同时，Clozapine也可以从它的N-氧化物代谢产物生成。换而言之，Clozapine和clozapine-N-oxide（CNO）间的代谢途径是可逆的[3]。在大鼠初级皮层细胞和SH-SY5Y神经母细胞瘤细胞中，给予200 ng/ml的clozapine-N-oxide（CNO）显著减少5-HT2受体密度[1]。在鉴定方法方面，反相HPLC已被报道可以检测人血浆中的Clozapine以及其两种主要代谢产物[4]。
参考文献：
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.
- 1. Qiaocheng Zhai, Yizhun Zeng, et al. "Time-restricted feeding entrains long-term behavioral changes through the IGF2-KCC2 pathway." iScience. 2022 Apr 18;25(5):104267. PMID: 35521538
- 2. Qingtao Sun, Jianping Zhang, et al. "Acetylcholine deficiency disrupts extratelencephalic projection neurons in the prefrontal cortex in a mouse model of Alzheimer's disease." Nat Commun. 2022 Feb 22;13(1):998. PMID: 35194025
- 3. Sean D. Stocker, Megan M. Wenner, et al. "Activation of the Organum Vasculosum of the Lamina Terminalis Produces a Sympathetically Mediated Hypertension." Hypertension. 2022 Jan;79(1):139-149. PMID: 34809435
- 4. Santhosh D, Sherman J, et al. "Harnessing region-specific neurovascular signaling to promote germinal matrix vessel maturation and hemorrhage prevention." Dis Model Mech. 2019 Oct 10. pii: dmm.041228. PMID: 31601549
- 5. 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):450. PMID: 31108875
- 6. Laura A DeNardo, Cindy D Liu, et al."Temporal Evolution of Cortical Ensembles Promoting Remote Memory Retrieval." bioRxiv. 2018 April 5.
| Storage | Store at -20°C |
| M.Wt | 342.82 |
| Cas No. | 34233-69-7 |
| Formula | C18H19ClN4O |
| Solubility | insoluble in EtOH; ≥17.15 mg/mL in DMSO; ≥49 mg/mL in H2O with gentle warming |
| Chemical Name | 3-chloro-6-(4-methyl-4-oxidopiperazin-4-ium-1-yl)-5H-benzo[b][1,4]benzodiazepine |
| SDF | Download SDF |
| Canonical SMILES | C[N+]1(CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl)[O-] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 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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质量控制和MSDS
- 批次:
化学结构
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