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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $30 | In Stock | |
5 mg | $45 | In Stock | |
10 mg | $76 | In Stock | |
25 mg | $126 | In Stock | |
50 mg | $187 | In Stock | |
100 mg | $278 | In Stock |
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] |
Molecular Weight | 342.82 |
Formula | C18H19ClN4O |
Cas No. | 34233-69-7 |
Smiles | CN1(=O)CCN(C=2C=3C(NC=4C(N2)=CC(Cl)=CC4)=CC=CC3)CC1 |
Relative Density. | 1.36g/cm3 |
Storage | Powder: -20°C for 3 years | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 1 mg/mL (2.92 mM), Sonication is recommended. ![]() Ethanol: 10 mg/mL (29.17 mM), Sonication is recommended. DMSO: 60 mg/mL (175.02 mM), The compound is unstable in solution, please use soon. ![]() | |||||||||||||||||||||||||||||||||||||||||||||
In Vivo Formulation | Saline: 25 mg/mL (72.92 mM), In vivo: Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.![]() | |||||||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||||||||||||
H2O/Ethanol/DMSO
Ethanol/DMSO
DMSO
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