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| CLOZAPINE N-OXIDE Basic information |
| Product Name: | CLOZAPINE N-OXIDE | | Synonyms: | e)(1,4)diazepine,8-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(n-oxide;CLOZAPINE N-OXIDE;8-CHLORO-11-[4-METHYL-1-PIPERAZINYL]-5H-DIBENZO[B,E][1,4]DIAZEPINE N-OXIDE;MAJORMETABOLITEOFCLOZAPINE.POSSESSESLITTLEORNOACTIVITYAT5-HTRECEPTORS;Clozapine N-oxide Methanol Adduct;Clozapine N-oxide solution;Clozapine N-oxide (CNO);8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine | | CAS: | 34233-69-7 | | MF: | C18H19ClN4O | | MW: | 342.82 | | EINECS: | | Product Categories: | Various Metabolites and Impurities;Metabolites | | Mol File: | 34233-69-7.mol |
| CLOZAPINE N-OXIDE Chemical Properties |
| Melting point | 190-248°C | | Fp | 9℃ | | storage temp. | -20°C Freezer, Under Inert Atmosphere | | solubility | Soluble in DMSO. | | form | powder | | pka | 6.86±0.20(Predicted) | | color | Yellow | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. | | InChIKey | OGUCZBIQSYYWEF-UHFFFAOYSA-N |
| CLOZAPINE N-OXIDE Usage And Synthesis |
| Description | Clozapine-N-oxide (34233-69-7) is a clozapine?metabolite1?which is pharmacologically inert2. Agonist at human muscarinic designer receptors known as DREADDs, (designer receptors exclusively activated by designer drug).2?May be used to control grafted human pluripotent stem cell-derived neurons engineered to express DREADDs.3,4??Numerous other applications.5,6 | | Chemical Properties | Yellow Solid | | Uses | Clozapine N-oxide has been used:- for the activation of human M4 muscarinic (hM4Di) in primary motor cortex
- for inducing in vivo chemogenetic manipulation and impairing locomotor activity in Th-cre transgenic mice
- in behavioral testing in mice and for stimulating (HEK293) cells
| | Uses | A 5-HT2 antagonist. A major metabolite of clozapine that can be monitored by HPLC. Possesses little or no activity towards serotonin receptors | | General Description | Clozapine N-oxide (CNO), inactive from of clozapine drug, activates G-protein-coupled receptors (GPCRs). CNO serves as a synthetic ligand for engineered human muscarinic receptor. It elicits clozapine-like effects upon metabolic conversion. Clozapine conversion to CNO favors its passage through blood-brain barrier. | | Biochem/physiol Actions | 5-HT2 serotonin receptor antagonist; major metabolite of clopazine that can be monitored by HPLC. | | References | 1) Eiermann?et al.?(1997),?The involvement of CYP1A2 and CYP3A4 in the metabolism of clozapine; Br. J. Clin. Pharmacol.,?44?439
2) 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. USA,?104?5163
3) Chen?et al.?(2016),?Chemical Control of Grafted Human PSC-Derived Neurons in a Mouse Model of Parkinson’s Disease; Cell Stem Cell,?18?817
4) Vazey and Aston-Jones (2014),?Designer receptors: therapeutic adjuncts to cell replacement therapy in Parkinson’s disease: J. Clin. Invest.,?124?2858
5) Gomez?et al.?(2017)?Chemogenetics revealed: DREADD occupancy and activation via converted clozapine; Science?357?503
6) Marcinkiewcz?et al. (2016)?Serotonin engages an anxiety and fear-promoting circuit in the extended amygdala; Nature?537?97 |
| CLOZAPINE N-OXIDE Preparation Products And Raw materials |
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