A metabolite of clozapine and muscarinic DREADD agonist
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Clozapine N-oxide (hydrochloride)

Item No. 25780

Technical Information
Formal Name
8-chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine, dihydrochloride
CAS Number
2250025-93-3
Synonyms
  • CNO
Molecular Formula
C18H19ClN4O • 2HCl
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 25 mg/mlDMSO: 25 mg/mlEthanol: 25 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
213, 226 nm
SMILES
C[N+]1(CCN(C2=NC(C=C(Cl)C=C3)=C3NC4=CC=CC=C24)CC1)[O-].Cl.Cl
InChi Code
InChI=1S/C18H19ClN4O.2ClH/c1-23(24)10-8-22(9-11-23)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18;;/h2-7,12,20H,8-11H2,1H3;2*1H
InChi Key
MBRGKRXDVKTUPT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Clozapine N-oxide is a major metabolite of clozapine (Item No. 12059) and an activator of designer receptors exclusively activated by designer drugs (DREADDs) derived from human muscarinic acetylcholine receptors (EC50s = 16.7, 323, 17.4, 18.3, and 18.7 nM for PASMCs expressing hM1-5D receptors, respectively).1,2 It prevents action potential firing in cultured hippocampal neurons transiently expressing hM4D receptors.2 Clozapine N-oxide increases glutamate in the nucleus accumbens core and inhibits cue-induced reinstatement of cocaine-seeking behavior in rats transfected with hM3Dq DREADD receptors.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Eiermann, B., Engel, G., Johansson, I., et alThe involvement of CYP1A2 and CYP3A4 in the metabolism of clozapine. Br. J. Clin. Pharmacol. 44(5), 439-446 (1997).

    2. Armbruster, B.N., Li, X., Pausch, M.H., et alEvolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand. PNAS 104(12), 5163-5168 (2007).

    3. Scofield, M.D., Boger, H.A., Smith, R.J., et alGq-DREADD selectively initiates glial glutamate release and inhibits cue-induced cocaine seeking. Biol. Psychiatry 78(7), 441-451 (2015).