Clozapine N-oxide

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Chemical Structure| 34233-69-7 同义名 : 氯氮平N-氧化 ;CNO
CAS号 : 34233-69-7
货号 : A685542
分子式 : C18H19ClN4O
纯度 : 99%
分子量 : 342.82
MDL号 : MFCD00210190
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(306.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(2.92 mM)，配合低频超声助溶
生物活性
靶点

  • Dopamine receptor
描述 Clozapine N-oxide, a primary metabolite of Clozapine, serves as an agonist for human muscarinic designer receptors (DREADDs), effectively activating DREADD receptors hM3Dq and hM4Di, and is capable of crossing the blood-brain barrier[1].[2].[3].[4]. Clozapine itself is known as a powerful antagonist of dopamine and a selective agonist for the muscarinic M4 receptor, with an EC50 value of 11 nM[5].[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.92mL

0.58mL

0.29mL

14.58mL

2.92mL

1.46mL

29.17mL

5.83mL

2.92mL
参考文献

[1]Wess J, et al. Novel designer receptors to probe GPCR signaling and physiology. Trends Pharmacol Sci. 2013 Jul;34(7):385-92.

[2]Manvich DF, et al. The DREADD agonist clozapine N-oxide (CNO) is reverse-metabolized to clozapine and produces clozapine-like interoceptive stimulus effects in rats and mice. Sci Rep. 2018 Mar 1;8(1):3840.

[3]van der Peet PL, et al. Gram scale preparation of clozapine N-oxide (CNO), a synthetic small molecule actuator for muscarinic acetylcholine DREADDs. MethodsX. 2018 Mar 23;5:257-267.

[4]Joseph Cichon, et al. Branch-specific dendritic Ca(2+) spikes cause persistent synaptic plasticity. Nature. 2015 Apr 9;520(7546):180-5.

[5]Silva RR, et al. Evaluation of Functional Selectivity of NSC 170973, Clozapine, and LASSBio-579, an Experimental Compound With Antipsychotic-Like Actions in Rodents, at G Protein and Arrestin Signaling Downstream of the Dopamine D2 Receptor. Front Pharmacol. 2019 Jun 4;10:628.

[6]Zorn SH, et al. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2.