1. GPCR/G Protein
    Neuronal Signaling
    Metabolic Enzyme/Protease
  2. Dopamine Receptor
    mAChR
    Drug Metabolite
  3. Clozapine (N-oxide)

Clozapine (N-oxide) 

Cat. No.: HY-17366 Purity: 99.98%
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Clozapine (N-oxide) is a pharmacologically inert metabolite of Clozapine, an antipsychotic drug. Clozapine (N-oxide) is a agonist for the DREADD (Designer Receptors Exclusively Activated by Designer Drug) system. Clozapine is a potent antagonist of dopamine. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).

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Clozapine (N-oxide) Chemical Structure

Clozapine (N-oxide) Chemical Structure

CAS No. : 34233-69-7

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Clozapine (N-oxide):

Top Publications Citing Use of Products

    Clozapine (N-oxide) purchased from MCE. Usage Cited in: Biol Psychiatry. 2017 May 1;81(9):737-747.

    c-fos immunoreactivity in the VTA 90 minutes after injections of 1 mg/kg Clozapine N-oxide (CNO).
    • Biological Activity

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    Description

    Clozapine (N-oxide) is a pharmacologically inert metabolite of Clozapine, an antipsychotic drug. Clozapine (N-oxide) is a agonist for the DREADD (Designer Receptors Exclusively Activated by Designer Drug) system[1][2]. Clozapine is a potent antagonist of dopamine. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[3][4].

    In Vivo

    After a single intraperitoneal (i.p.) injection of Clozapine N-oxide (1 mg/kg) into mice, Clozapine N-oxide (CNO) plasma levels peak at 15 min and are very low after 2 h. Acutely administered CNO can be metabolically converted to Clozapine in other species such as human and guinea-pig. The metabolites that may form after chronic administration of CNO to DREADD-expressing mice (or other species) have not been studied systematically. However, even if back-transformation to Clozapine occurs after chronic CNO administration, it should be noted that Clozapine is a more potent (by ~10-fold) DREADD agonist than CNO itself. Moreover, confounding biological effects of potential CNO metabolites can be easily identified by including both saline- and CNO-treated WT animals in a particular DREADD study. Despite the short plasma half-life of CNO in mice, the biological effects that have been described after acute treatment of DREADD-expressing experimental animals are usually much longer (6-10 h). One possibility is that CNO tends to accumulate in tissues, although other scenarios are also feasible[1]. Using a general pharmacokinetic model for the interconversion process, the mean total clearances of Clozapine and Clozapine N-oxide (CNO) are 28.45 L/hr and 45.30 L/hr, respectively[2].

    Molecular Weight

    342.82

    Formula

    C₁₈H₁₉ClN₄O

    CAS No.

    34233-69-7

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (291.70 mM)

    Methanol : ≥ 28.6 mg/mL (83.43 mM)

    H2O : 1 mg/mL (2.92 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9170 mL 14.5849 mL 29.1698 mL
    5 mM 0.5834 mL 2.9170 mL 5.8340 mL
    10 mM 0.2917 mL 1.4585 mL 2.9170 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (7.29 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (7.29 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.98%

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    Keywords:

    Clozapine (N-oxide)Dopamine ReceptormAChRDrug MetaboliteMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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