Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 30.00 | |
5 mg | In stock | $ 45.00 | |
10 mg | In stock | $ 76.00 | |
25 mg | In stock | $ 126.00 | |
50 mg | In stock | $ 187.00 | |
100 mg | In stock | $ 278.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 50.00 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 1 mg/mL
Ethanol: 10 mg/mL
DMSO: 6 mg/mL, The compound is unstable in solution, please use soon.
You can also refer to dose conversion for different animals. More
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CLOZAPINE N-OXIDE 34233-69-7 GPCR/G Protein Metabolism Neuroscience Dopamine Receptor 5-HT Receptor Drug Metabolite AChR Clozapine N-oxide BBB DREADDs hM3Dq metabolite inhibit Inhibitor CLOZAPINE N OXIDE Clozapine G-protein Muscarinic acetylcholine receptor mAChR muscarinic-M4 CLOZAPINE NOXIDE inhibitor