Catalog Number: 4936
Chemical Name: 8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Biological Activity
Metabolite of clozapine (Cat. No. 0444). Activates human muscarinic designer receptors (DREADDs) in vitro. Silences hippocampal neurons expressing hM4 DREADDs in vitro. Activates Gs-linked DREADDS- AgRP in mice via intracerebroventricular (i.c.v) injection. Shown to be a P-glycoprotein (P-gp) efflux pump substrate. Water soluble salt (Cat.No.6329) also available. Other potent and selective hM3Dq DREADD agonists available: DREADD agonist 21 (Cat. No. 5548) and Perlapine (Cat. No. 5549)
Technical Data
  • M.Wt:
    342.82
  • Formula:
    C18H19ClN4O
  • Solubility:
    Soluble to 20 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    34233-69-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. The involvement of CYP1A2 and CYP3A4 in the metabolism of clozapine.
    Eiermann et al.
    Br.J.Clin.Pharmacol., 1997;44:439
  2. Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand.
    Armbruster et al.
    Proc.Natl.Acad.Sci.U.S.A., 2007;104:5163
  3. LMO4 is essential for paraventricular hypothalamic neuronal activity and calcium channel expression to prevent hyperphagia.
    Zaman et al.
    J.Neurosci., 2014;34:140
  4. Chemogenetics revealed: DREADD occupancy and activation via converted clozapine.
    Gomez et al.
    Science, 2017;357:503
  5. Gs-coupled GPCR signalling in AgRP neurons triggers sustained increase in food intake.
    Nakajima et al.
    Nat. Commun., 2016;8:10268
  6. DREADDs for Neuroscientists
    Roth et al.
    Neuron, 2016;89:683
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Clozapine N-oxide include:

2 Citations: Showing 1 - 2
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  1. Appetite controlled by a cholecystokinin nucleus of the solitary tract to hypothalamus neurocircuit.
    Authors: D'Agostino Et al.
    PLoS Biol 2016;5
  2. Ethanol-seeking behavior is expressed directly through an extended amygdala to midbrain neural circuit
    Authors: Pina and Cunningham Et al.
    Neurobiology of Learning and Memory 2016;137:83
Tocris Small Molecules
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Clozapine

0444 11  
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