| Name | Clozapine N-Oxide |
| Description | Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist. |
| In vitro | METHODS: hM4Di-transduced primary embryonic rat neuronal cultures were treated with Clozapine N-oxide (0.01-1000 nM), and activity on hM4Di receptors was detected by FLIPR assay.
RESULTS: The EC50 value for Clozapine N-oxide was 8.1 nM. [1]
METHODS: WT and hM3Dq-transfected mouse embryoma cells ATDC5 were treated with Clozapine N-oxide (750 nM) to detect intracellular calcium signaling.
RESULTS: Administration of Clozapine N-oxide resulted in immediate coordinated induction of single [Ca2+]i spines in hM3Dq-ATDC5 cells, and only spontaneous [Ca2+]i signaling was observed in Clozapine N-oxide-treated WT controls. [2] |
| In vivo | METHODS: To investigate potential effects on sleep, Clozapine N-oxide (1-10 mg/kg) was injected intraperitoneally into C57BL/6J mice.
RESULTS: Clozapine N-oxide altered sleep in mice. Sleep was analyzed using electroencephalography (EEG) and electromyography (EMG), revealing dose-dependent suppression of rapid eye movement (REM) sleep, changes in EEG spectral power during non-rapid eye movement (NREM) sleep, and alterations in sleep structure. [3]
METHODS: To investigate the effects on reward-seeking behavior, Clozapine N-oxide (0.1-10 mg/kg) was administered intraperitoneally to C57BL6/JJcl mice.
RESULTS: The off-target effects of commonly used doses of Clozapine N-oxide on motivated reward seeking were negligible. [4] |
| Storage | The compound is unstable in solution. Please use soon | Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Saline : 25 mg/mL (72.92 mM), Solution. The compound is unstable in solution, please use soon.
H2O : 1 mg/mL (2.92 mM), Sonication is recommended. The compound is unstable in solution, please use soon.
Ethanol : 10 mg/mL (29.17 mM), Sonication is recommended. The compound is unstable in solution, please use soon.
DMSO : 252.5 mg/mL (736.54 mM), Sonication is recommended. The compound is unstable in solution, please use soon.
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| Keywords | muscarinic-M4 | Muscarinic acetylcholine receptor | metabolite | mAChR | Inhibitor | inhibit | hM3Dq | G-protein | DrugMetabolite | Drug Metabolite | DREADDs | DopamineReceptor | Dopamine Receptor | Dopamine | Clozapine N-oxide | CLOZAPINE N-OXIDE | CLOZAPINE NOXIDE | CLOZAPINE N OXIDE | Clozapine | BBB | 5HTReceptor | 5HT Receptor | 5-HT |
| Inhibitors Related | Adiphenine hydrochloride | Alverine citrate | Dapoxetine hydrochloride | Mycophenolate Mofetil | Urethane | Ribavirin | Octopamine hydrochloride | Isonicotinic acid | Choline chloride | Propoxur | Lansoprazole sulfide | 4-(4-Amino-3-fluorophenoxy)-N-methylpicolinamide |
United States
