Clozapine

Pricing Availability Delivery Time Qty
Cat.No. 0444 - Clozapine | C18H19ClN4 | CAS No. 5786-21-0
Description: Dopamine antagonist with some D4 selectivity. Also 5-HT2A/2C antagonist
Chemical Name: 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥99% (HPLC)
Datasheet
Citations (11)
Literature

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).

Technical Data

M. Wt 326.83
Formula C18H19ClN4
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 5786-21-0
PubChem ID 2818
InChI Key ZUXABONWMNSFBN-UHFFFAOYSA-N
Smiles CN1CCN(CC1)C1=NC2=C(NC3=C1C=CC=C3)C=CC(Cl)=C2

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
2eq.HCl 16.34 50mM with gentle warming
DMSO 32.68 100
ethanol 16.34 50

Preparing Stock Solutions

The following data is based on the product molecular weight 326.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.06 mL 15.3 mL 30.6 mL
5 mM 0.61 mL 3.06 mL 6.12 mL
10 mM 0.31 mL 1.53 mL 3.06 mL
50 mM 0.06 mL 0.31 mL 0.61 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

Seeman and Van Tol (1994) Dopamine receptor pharmacology. Trends Pharmacol.Sci. 15 264 PMID: 7940991

Jensen et al (2013) esign, 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 J.Med.Chem. 56 1211 PMID: 23301527


If you know of a relevant reference for Clozapine, please let us know.

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Keywords: Clozapine, supplier, Dopamine, antagonists, D4, selectivity, 5HT2A/2C, Non-Selective, Receptors, Serotonin, 5HT2C, 5HT2, 5HT2A, dopaminergic, Non-selective, Dopamine, 5-HT2A, Receptors, 5-HT2C, Receptors, Non-selective, Dopamine, Tocris Bioscience

11 Citations for Clozapine

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

Chau et al (2013) Pramipexole reduces phosphorylation of α-synuclein at serine-129. Exp Mol Med 51 573 PMID: 23681749

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

Balu et al (2008) Differential regulation of central BDNF protein levels by antidepressant and non-antidepressant drug treatments. J Mol Neurosci 1211 37 PMID: 18433734

Roh et al (2007) Haloperidol and clozapine differentially regulate signals upstream of glycogen synthase kinase 3 in the rat frontal cortex. Front Cell Neurosci 39 353 PMID: 17603289

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

Griebel et al (2016) The mGluR2 positive allosteric modulator, SAR218645, improves memory and attention deficits intranslational models of cognitive symptoms associated with schizophrenia Scientific Reports 6 35320 PMID: 27734956

Canfrán-Duque et al (2015) Curcumin Mitigates the Intracellular Lipid Deposit Induced by Antipsychotics In Vitro. Int J Tryptophan Res 10 e0141829 PMID: 26517556

Larsson et al (2015) Chronic Antipsychotic Treatment in the Rat - Effects on Brain Interleukin-8 and Kynurenic Acid. Brain Res 8 49 PMID: 26448689


Do you know of a great paper that uses Clozapine from Tocris? If so please let us know.

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