Customer Validation
- •Biol Psychiatry. 2017 May 1;81(9):737-747.
| Description |
Clozapine N-oxide is a pharmacologically inert metabolite of Clozapine, which is a potent 5-HT1C receptor antagonist. Clozapine N-oxide (CNO) is a DREADD (designer receptors exclusively activated by designer drug) agonist. |
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| 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]. |
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| Preparing Stock Solutions |
Please refer to the solubility information to select the appropriate solvent.
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| References |
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| Molecular Weight |
342.82 |
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| Formula |
C₁₈H₁₉ClN₄O |
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| CAS No. |
34233-69-7 |
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| Storage |
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| Shipping | Room temperature in continental US; may vary elsewhere |
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| Solvent & Solubility |
10 mM in DMSO
* "<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation=""> |
Purity: 99.98%
COA (96 KB) HNMR (290 KB) RP-HPLC (175 KB)
Handling Instructions (1252 KB)-
[1]. Wess J, et al. Novel designer receptors to probe GPCR signaling and physiology. Trends Pharmacol Sci. 2013 Jul;34(7):385-92.
[2]. Chang WH, et al. Reversible metabolism of clozapine and clozapine N-oxide in schizophrenic patients. Prog Neuropsychopharmacol Biol Psychiatry. 1998 Jul;22(5):723-39.
