Clozapine N-oxide (Standard)

Clozapine N-oxide (Standard) is the analytical standard of Clozapine N-oxide. This product is intended for research and analytical applications. Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide cannot cross the blood-brain barrier[1][2][3][4]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist[5][6].

Product Specifications

CAS Number

[34233-69-7]

UNSPSC

12352005

Hazard Statement

H301, H336

Target

Dopamine Receptor; Drug Metabolite; mAChR; Reference Standards

Related Pathways

GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling; Others

Field of Research

Neurological Disease

Purity

99.78

Smiles

[O-][N+]1(C)CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42)CC1

Molecular Formula

C18H19ClN4O

Molecular Weight

342.82

Precautions

H301, H336

References & Citations

[1]Wess J, et al. Novel designer receptors to probe GPCR signaling and physiology. Trends Pharmacol Sci. 2013 Jul;34 (7) :385-92.|[2]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.|[3]Zorn SH, et al. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269 (3) :R1-2.|[4]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.|[5]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.|[6]Joseph Cichon, et al. Branch-specific dendritic Ca (2+) spikes cause persistent synaptic plasticity. Nature. 2015 Apr 9;520 (7546) :180-5.