Cat. No. 0444
Chemical Name: 8-Chloro-11-(4-methyl-1-piperazinyl
Biological ActivityAtypical 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).
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.
Certificate of Analysis / Safety Data Sheet
Jensen et al (2013) 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 properties. J.Med.Chem. 56 1211. PMID: 23301527.
Seeman and Van Tol (1994) Dopamine receptor pharmacology. Trends Pharmacol.Sci. 15 264. PMID: 7940991.
Ellenbroek et al (1991) The involvement of dopamine D1 and D2 receptors in the effects of the classical neuroleptic haloperidol and the atypical neuroleptic clozapine. Eur.J.Pharmacol. 196 103. PMID: 1678712.
Canton et al (1990) Binding of typical and atypical antipsychotics to 5-HT1C and 5-HT2 sites: clozapine potently interacts with 5-HT1C sites. Eur.J.Pharmacol. 191 93. PMID: 1982659.
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Citations are publications that use Tocris products. Selected citations for Clozapine include:
Jia et al (2013) Age-dependent regulation of synaptic connections by dopamine D2 receptors. Nat Neurosci 16 1627. PMID: 24121738.
Hillenmeyer et al (2010) Systematic analysis of genome-wide fitness data in yeast reveals novel gene function and drug action. Genome Biol 11 R30. PMID: 20226027.
Magliaro and Saldanha (2009) 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. Brain Res 1283 14. PMID: 19501068.
Oliver and Davies (2009) Interaction between environmental and genetic factors modulates schizophrenic endophenotypes in the Snap-25 mouse mutant blind-drunk. Hum Mol Genet 18 4576. PMID: 19729413.
Sur et al (2003) N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity. Proc Natl Acad Sci U S A 100 13674. PMID: 14595031.
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Keywords: Clozapine, supplier, Dopamine, antagonists, D4, selectivity, 5HT2A/2C, Non-Selective, Receptors, Serotonin, 5HT2C, 5HT2, 5HT2A, dopaminergic, Tocris Bioscience, Non-selective Dopamine Antagonist products
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