Clozapine N-oxide - CAS 34233-69-7
Catalog number:
Not Intended for Therapeutic Use. For research use only.
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Molecular Weight:
5-HT Receptor
Clozapine N-oxide is a major metabolite of clozapine that can be detected in the earliest excretion time interval after clozapine administration. It is produced by the action of cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4, whose activities, in turn,
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Yellow solid
3-chloro-6-(4-methyl-4-oxidopiperazin-4-ium-1-yl)-5H-benzo[b][1,4]benzodiazepine; 8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine;
Soluble in DMSO
Store at -20 °C
A 5-HT2 antagonist. A major metabolite of clozapine that can be monitored by HPLC. Possesses little or no activity towards serotonin receptors.
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
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1.Chemogenetic inhibition of cells in the paramedian midbrain tegmentum increases locomotor activity in rats.
Wirtshafter D1, Stratford TR2. Brain Res. 2016 Feb 1;1632:98-106. doi: 10.1016/j.brainres.2015.12.014. Epub 2015 Dec 17.
Pronounced hyperactivity can be produced by lesions or pharmacological inhibition of cells in the median raphe nucleus (MR) located in the paramedian midbrain tegmentum. In the current study we examined whether a similar effect can be seen after chemogenetic inhibition of cells in this region using the DREADD (Designer Receptors Exclusively Activated by Designer Drugs) approach. We found that the DREADD ligand clozapine-N-oxide (CNO) increased locomotor activity in animals expressing the inhibitory DREADD hM4Di, but not those injected with a control virus in the MR. The effect was of rapid onset and short duration and persisted for at least four months after virus injections. Histological examination of the brains indicated that labeled fibers followed the known projection patterns of the MR to a variety of forebrain and midbrain structures. These findings confirm the role of the MR region in the control of locomotion and suggest that the DREADD technique may be a useful approach to the study of the functional architecture of this complex area.
2.Inactivation of the lateral orbitofrontal cortex increases drinking in ethanol-dependent but not non-dependent mice.
Hartog CD1, Zamudio-Bulcock P1, Nimitvilai S1, Gilstrap M1, Fedarovich H1, Motts A1, Woodward JJ2. Neuropharmacology. 2016 Mar 22. pii: S0028-3908(16)30103-4. doi: 10.1016/j.neuropharm.2016.03.031. [Epub ahead of print]
Long-term consumption of ethanol affects cortical areas that are important for learning and memory, cognition, and decision-making. Deficits in cortical function may contribute to alcohol-abuse disorders by impeding an individual's ability to control drinking. Previous studies from this laboratory show that acute ethanol reduces activity of lateral orbitofrontal cortex (LOFC) neurons while chronic exposure impairs LOFC-dependent reversal learning and induces changes in LOFC excitability. Despite these findings, the role of LOFC neurons in ethanol consumption is unknown. To address this issue, we examined ethanol drinking in adult C57Bl/6J mice that received an excitotoxic lesion or viral injection of the inhibitory DREADD (designer receptor exclusively activated by designer drug) into the LOFC. No differences in ethanol consumption were observed between sham and lesioned mice during access to increasing concentrations of ethanol (3-40%) every other day for 7 weeks.
3.Muscarinic Control of Rostromedial Tegmental Nucleus GABA Neurons and Morphine-induced Locomotion.
Wasserman DI1, Tan JM1, Kim JC1, Yeomans JS1. Eur J Neurosci. 2016 Mar 17. doi: 10.1111/ejn.13237. [Epub ahead of print]
Opioids induce rewarding and locomotor effects by inhibiting rostromedial tegmental GABA neurons that express μ-opioid and nociceptin receptors. These GABA neurons then strongly inhibit dopamine neurons. Opioid-induced reward, locomotion, and dopamine release also depend on pedunculopontine and laterodorsal tegmental cholinergic and glutamate neurons, many of which project to and activate ventral tegmental area dopamine neurons. Here we show that laterodorsal tegmental and pedunculopontine cholinergic neurons project to both rostromedial tegmental nucleus and ventral tegmental area, and that M4 muscarinic receptors are co-localized with μ-opioid receptors associated with rostromedial tegmental GABA neurons. To inhibit or excite rostromedial tegmental GABA neurons, we utilized adeno-associated viral vectors and DREADDs to express designed muscarinic receptors (M4D or M3D respectively) in GAD2::Cre mice. In M4D-expressing mice, clozapine-N-oxide increased morphine-induced, but not vehicle-induced, locomotion.
4.A G Protein-biased Designer G Protein-coupled Receptor Useful for Studying the Physiological Relevance of Gq/11-dependent Signaling Pathways.
Hu J1, Stern M1, Gimenez LE2, Wanka L3, Zhu L1, Rossi M1, Meister J1, Inoue A4, Beck-Sickinger AG3, Gurevich VV2, Wess J5. J Biol Chem. 2016 Apr 8;291(15):7809-20. doi: 10.1074/jbc.M115.702282. Epub 2016 Feb 5.
Designerreceptorsexclusivelyactivated by adesignerdrug (DREADDs) are clozapine-N-oxide-sensitive designer G protein-coupled receptors (GPCRs) that have emerged as powerful novel chemogenetic tools to study the physiological relevance of GPCR signaling pathways in specific cell types or tissues. Like endogenous GPCRs, clozapine-N-oxide-activated DREADDs do not only activate heterotrimeric G proteins but can also trigger β-arrestin-dependent (G protein-independent) signaling. To dissect the relative physiological relevance of G protein-mediatedversusβ-arrestin-mediated signaling in different cell types or physiological processes, the availability of G protein- and β-arrestin-biased DREADDs would be highly desirable. In this study, we report the development of a mutationally modified version of a non-biased DREADD derived from the M3muscarinic receptor that can activate Gq/11with high efficacy but lacks the ability to interact with β-arrestins.
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CAS 34233-69-7 Clozapine N-oxide

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