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Clozapine N-oxide
SKU
HY-17366-10 mg
Category Reference compound
Tags Dopamine Receptor;Drug Metabolite;mAChR, GPCR/G Protein;Metabolic Enzyme/Protease;Neuronal Signaling, Neurological Disease
$58 – $95
Products Details
Product Description
– 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 can 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].
Web ID
– HY-17366
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C18H19ClN4O
Citations
– Acta Pharmacol Sin. 2023 Jan 25.|Acta Physiol. 2023 Jan 4;e13917.|Adv Sci (Weinh). 2023 Apr 14;e2204824.|Adv Sci (Weinh). 2023 Jun 16;e2301110.|Anesthesiology. 2021 Jul 13.|Anesthesiology. 2021 Jul 16.|Biol Psychiatry. 2017 May 1;81(9):737-747.|bioRxiv. 2023 Oct 9.|Brain Behav Immun. 2023 Jun 5;S0889-1591(23)00141-1.|Brain Commun. 30 August 2022.|Cell Metab. 2022 Feb 1;34(2):285-298.e7.|Cell Rep. 2021 Mar 23;34(12):108889.|Cell Rep. 2023 Dec 3;42(12):113551.|Cell Rep. 2023 Mar 21;42(4):112290.|CNS Neurosci Ther. 2022 Nov 15.|Commun Biol. 2021 Sep 16;4(1):1088.|Commun Biol. 2023 Jan 14;6(1):50.|Ecotoxicol Environ Saf. 2023 Jun 29;262:115205.|Elife. 2021 Sep 16;10:e67535.|FASEB J. 2020 Sep;34(9):11913-11924.|Front Cell Neurosci. 2021 Apr 30;15:671473.|Front Neurosci. 2020 Jul 14;14:646.|iScience. 2023 Aug 14.|iScience. 2023 Oct 20.|J Neuroinflammation. 2022 Jun 27;19(1):166.|J Neuroinflammation. 2022 May 27;19(1):123.|J Neuropathol Exp Neurol. 2023 Jul 21;nlad056.|J Neurosci. 2021 Oct 11;JN-RM-0881-21.|Life Metabolism. 2023 Feb 4.|Life Sci. 2020 Oct 1;258:118099.|Nat Commun. 2020 Jun 5;11(1):2847. |Nat Commun. 2020 Nov 27;11(1):6045.|Nat Commun. 2022 Apr 25;13(1):2233.|Nat Commun. 2023 Apr 17;14(1):2182.|Nat Neurosci. 2022 Nov 17.|Nat Neurosci. 2023 Apr;26(4):542-554.|Neural Regen Res. 2024 Feb;19(2):425-433.|Neurobiol Dis. 2023 May 12;106155.|Neurobiol Stress. 22 September 2022, 100492.|Neuropharmacology. 2018 Jun;135:474-486.|Neuropsychopharmacology. 2022 Dec 16.|Neurosci Bull. 2021 Jun 18.|Neurosci Bull. 2021 May;37(5):597-610.|Neurosci Bull. 2022 Nov 7.|Neurosci Bull. 2023 Jan 11.|Neuroscience. 2019 Aug 21;414:299-310. |P Natl Acad Sci USA. 13, 2021 118 (28) e2103505118.|Proc Natl Acad Sci U S A. 2019 Aug 13;116(33):16583-16592.|Proc Natl Acad Sci U S A. 2023 May 9;120(19):e2215590120.|Prog Neuropsychopharmacol Biol Psychiatry. 18 December 2021, 110496.|Psychoneuroendocrinology. 2020 Jul;117:104690.|Research Square Preprint. 2021 Mar.|Research Square Preprint. 2023 Sep 22.|Research Square Print. September 6th, 2022|SSRN. 2023 Jul 18.|Theranostics. 2023 May 11;13(9):2946-2961.|Transl Psychiatry. 2020 Jun 20;10(1):202.|University of Michigan, Horace H. Rackham School of Graduate Studies. 2018 Oct.|Cells. 2022 Dec 21;12(1):26.|Cells. 2023, 12(1), 26.|iScience. 2022: 105840.|Pharmacol Res. 2023 Apr 15;106773.
References
– [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.
CAS Number
– 34233-69-7
Molecular Weight
– 342.82
Compound Purity
– 99.98
SMILES
– [O-][N+]1(C)CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42)CC1
Clinical Information
– No Development Reported
Research Area
– Neurological Disease
Solubility
– DMSO : 100 mg/mL (ultrasonic)|H2O : 1 mg/mL (ultrasonic)
Target
– Dopamine Receptor;Drug Metabolite;mAChR
Isoform
– mAChR3;mAChR4
Pathway
– GPCR/G Protein;Metabolic Enzyme/Protease;Neuronal Signaling
Product type
– Reference compound
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