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Submit ReviewClozapine N-oxide
说明： Activator of hM3Dq and hM4Di DREADDs
别名： CNO
化学名： 8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
纯度： ≥99% (HPLC)
生物活性 for Clozapine N-oxide
Clozapine N-oxide is a synthetic ligand for human muscarinic engineered receptors, designer receptors activated by designer drugs (DREADD). Binds and activates hM3Dq and hM4Di DREADDs in vitro and in vivo. Metabolite of Clozapine (Cat. No. 0444). Shown to be a P-glycoprotein (P-gp) efflux pump substrate.
Example Applications of Clozapine N-oxide (CNO):
- Silences hippocampal neurons expressing hM4Di DREADDs in vitro
- Inhibits locomotor activity of mice expressing hM3Dq in GABAergic VTA neurons
- Inhibits short term memory retrieval in mice expressing hM4Di in hippocampal neurons
- Induces heat and mechanical hypersensitivity in mice expressing hM4Di in enkephalinergic neurons in the right lumbar dorsal horn
- Inhibits markers of social aggression in mice expressing hM4Di in hippocampal CA2 neurons
Alternative potent and selective hM3Dq and hM4Di DREADD agonists available: Deschloroclozapine and DREADD agonist 21
Water soluble salt also available.
This product contains 1 molar equivalent of ethanol.
技术数据 for Clozapine N-oxide
| 分子量 | 342.82 |
| 公式 | C18H19ClN4O |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 34233-69-7 |
| PubChem ID | 2819 |
| InChI Key | WYRDWWAASBTJLM-UHFFFAOYSA-N |
| Smiles | ClC(C=C3)=CC1=C3NC(C=CC=C2)=C2C(N4CC[N+](C)([O-])CC4)=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Clozapine N-oxide
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 6.86 | 20 |
制备储备液 for Clozapine N-oxide
以下数据基于产品分子量 342.82。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 14.58 mL | 72.92 mL | 145.85 mL |
| 1 mM | 2.92 mL | 14.58 mL | 29.17 mL |
| 2 mM | 1.46 mL | 7.29 mL | 14.58 mL |
| 10 mM | 0.29 mL | 1.46 mL | 2.92 mL |
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产品说明书 for Clozapine N-oxide
参考文献 for Clozapine N-oxide
参考文献是支持产品生物活性的出版物。
Eiermann et al (1997) The involvement of CYP1A2 and CYP3A4 in the metabolism of cloz. Br.J.Clin.Pharmacol. 44 439 PMID: 9384460
Armbruster et al (2007) 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. 104 5163 PMID: 17360345
Zaman et al (2014) LMO4 is essential for paraventricular hypothalamic neuronal activity and calcium channel expression to prevent hyperphagia. J.Neurosci. 34 140 PMID: 24381275
Gomez et al (2017) Chemogenetics revealed: DREADD occupancy and activation via converted cloz. Science 357 503 PMID: 28774929
Nakajima et al (2016) Gs-coupled GPCR signalling in AgRP neurons triggers sustained increase in food intake. Nat.Commun. 8 10268 PMID: 26743492
Roth (2016) DREADDs for Neuroscientists. Neuron 89 683 PMID: 26889809
If you know of a relevant reference for Clozapine N-oxide, please let us know.
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关键词: Clozapine N-oxide, Clozapine N-oxide supplier, clozapine, metabolite, clozapine-N-oxide, DREADDs, DREADD, Ligands, muscarnic, receptors, designer, CNO, chemogenetics, Multidrug, Transporters, Non-selective, Muscarinics, 4936, Tocris Bioscience
139 篇 Clozapine N-oxide 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Clozapine N-oxide 的部分引用包括：
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By
Anonymous on 06/15/2020
分析类型： In Vivo
种属： Mouse
细胞系/组织： neuron
1 mg/kg
Highly soluble and stable.
By
Anonymous on 01/04/2018
分析类型： Ex Vivo
种属： Mouse
Soluble in 0.9% saline. Perfused in brain slice experiment with patch clamp study.
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