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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 | Saline: 25 mg/mL (72.92 mM) H2O: 1 mg/mL (2.92 mM), Sonication is recommended. Ethanol: 10 mg/mL DMSO: 60 mg/mL (175.02 mM), The compound is unstable in solution, please use soon. | |||||||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||||||||||||
H2O/Saline/DMSO
Saline/DMSO
DMSO
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