Catalog Number: 0444
Chemical Name: 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Biological Activity

Atypical antipsychotic drug, with a much lower tendency to cause extrapyramidal side effects than conventional neuroleptics. Displays a broad range of pharmacological actions; the antipsychotic effects are thought to be mediated principally by 5-HT2A/2C and dopamine receptor blockade (Ki values are 21, 170, 170, 230 and 330 nM for D4, D3, D1, D2 and D5 receptors respectively).

Deuterated analog also available.
Technical Data
  • M.Wt:
    326.83
  • Formula:
    C18H19ClN4
  • Solubility:
    Soluble to 100 mM in DMSO and to 50 mM in 2eq.HCl with gentle warming
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    5786-21-0
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.
Additional Information
Other Product-Specific Information:
Background References
  1. Binding of typical and atypical antipsychotics to 5-HT1C and 5-HT2 sites: clozapine potently interacts with 5-HT1C sites.
    Canton et al.
    Eur.J.Pharmacol., 1990;191:93
  2. The involvement of dopamine D1 and D2 receptors in the effects of the classical neuroleptic haloperidol and the atypical neuroleptic clozapine.
    Ellenbroek et al.
    Eur.J.Pharmacol., 1991;196:103
  3. Dopamine receptor pharmacology.
    Seeman and Van Tol
    Trends Pharmacol.Sci., 1994;15:264
  4. Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-dazepin-3-ol analogues: novel 5-HT2A/5-HT2C receptor agonists with pro-cognitive
    Jensen et al.
    J.Med.Chem., 2013;56:1211
Citations:

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

11 Citations: Showing 1 - 10
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  1. The mGluR2 positive allosteric modulator, SAR218645, improves memory and attention deficits intranslational models of cognitive symptoms associated with schizophrenia
    Authors: Griebel Et al.
    Scientific Reports 2016;6:35320
  2. Chronic Antipsychotic Treatment in the Rat - Effects on Brain Interleukin-8 and Kynurenic Acid.
    Authors: Larsson Et al.
    Brain Res 2015;8:49
  3. Curcumin Mitigates the Intracellular Lipid Deposit Induced by Antipsychotics In Vitro.
    Authors: Canfrán-Duque Et al.
    Int J Tryptophan Res 2015;10:e0141829
  4. Pramipexole reduces phosphorylation of α-synuclein at serine-129.
    Authors: Chau Et al.
    Exp Mol Med 2013;51:573
  5. Age-dependent regulation of synaptic connections by dopamine D2 receptors.
    Authors: Jia Et al.
    Nat Neurosci 2013;16:1627
  6. Systematic analysis of genome-wide fitness data in yeast reveals novel gene function and drug action.
    Authors: Hillenmeyer Et al.
    Genome Biol 2010;11:R30
  7. Interaction between environmental and genetic factors modulates schizophrenic endophenotypes in the Snap-25 mouse mutant blind-drunk.
    Authors: Oliver and Davies
    Hum Mol Genet 2009;18:4576
  8. Clozapine protects PC-12 cells from death due to oxidative stress induced by hydrogen peroxide via a cell-type specific mechanism involving inhibition of extracellular signal-regulated kinase phosphorylation.
    Authors: Magliaro and Saldanha
    Brain Res 2009;1283:14
  9. Differential regulation of central BDNF protein levels by antidepressant and non-antidepressant drug treatments.
    Authors: Balu Et al.
    J Mol Neurosci 2008;1211:37
  10. Haloperidol and clozapine differentially regulate signals upstream of glycogen synthase kinase 3 in the rat frontal cortex.
    Authors: Roh Et al.
    Front Cell Neurosci 2007;39:353
  11. N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity.
    Authors: Sur Et al.
    Proc Natl Acad Sci U S A 2003;100:13674
Expand to show all 11 Citations
Tocris Small Molecules
Description Application Cat# Citations Images  

Clozapine N-oxide

4936 2  
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Clozapine - d8

5530  
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