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Biological Activity for Clozapine
Clozapine is an 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 for Clozapine
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Clozapine
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|2eq.HCl||16.34||50 with gentle warming|
Preparing Stock Solutions for Clozapine
The following data is based on the product molecular weight 326.83. Batch specific molecular weights may vary from batch to batch due to the degree 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|
References for Clozapine
References are publications that support the biological activity of the product.
Canton et al (1990) Binding of typical and atypical antipsychotics to 5-HT1C and 5-HT2 sites: cloz. potently interacts with 5-HT1C sites. Eur.J.Pharmacol. 191 93 PMID: 1982659
Ellenbroek et al (1991) The involvement of DA D1 and D2 receptors in the effects of the classical neuroleptic halope. and the atypical neuroleptic cloz. Eur.J.Pharmacol. 196 103 PMID: 1678712
Seeman and Van Tol (1994) DA receptor pharmacology. Trends Pharmacol.Sci. 15 264 PMID: 7940991
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 J.Med.Chem. 56 1211 PMID: 23301527
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Keywords: Clozapine, Clozapine supplier, Dopamine, antagonists, D4, selectivity, 5HT2A/2C, Non-Selective, Receptors, Serotonin, 5HT2C, 5HT2, 5HT2A, dopaminergic, Non-selective, 5-HT2A, 5-HT2C, 0444, Tocris Bioscience
20 Citations for Clozapine
Citations are publications that use Tocris products. Selected citations for Clozapine include:
Maldonado et al (2020) Oxytocin Shapes Spontaneous Activity Patterns in the Developing Visual Cortex by Activating Somatostatin Interneurons Curr Biol
Joshi and Panicker (2019) Identifying the In Vivo Cellular Correlates of Antipsychotic Drugs. Eneuro 5 PMID: 30713996
Hampson et al (2007) Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs. Diabetologia 50 1743 PMID: 17579833
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
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
Roh et al (2007) Haloperidol and cloz. differentially regulate signals upstream of glycogen synthase kinase 3 in the rat frontal cortex. Front Cell Neurosci 39 353 PMID: 17603289
Peng et al (2018) 5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology. Cell 172 719 PMID: 29398112
Cui et al (2016) Disrupted-in-schizophrenia1 (DISC1) L100P mutation alters synaptic transmission and plasticity in the hippocampus and causes recognition memory deficits. Mol Brain 9 89 PMID: 27729083
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
Herwerth et al (2012) D4 DA receptors modulate NR2B NMDA receptors and LTP in stratum oriens of hippocampal CA1. Cereb Cortex 22 1786 PMID: 21955919
Kurita et al (2012) HDAC2 regulates atypical antipsychotic responses through the modulation of mGlu2 promoter activity. Nat Neurosci 15 1245 PMID: 22864611
Singh et al (2009) Activation of the JAK-STAT pathway is necessary for desensitization of 5-HT2A receptor-stimulated phospholipase C signalling by olanzapine, cloz. and MDL 100907. Int J Neuropsychopharmacol 12 651 PMID: 18976543
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-MthD.-aspartate receptor activity. Proc Natl Acad Sci U S A 100 13674 PMID: 14595031
Chau et al (2013) Pramipexole reduces phosphorylation of α-synuclein at serine-129. Exp Mol Med 51 573 PMID: 23681749
Jia et al (2013) Age-dependent regulation of synaptic connections by DA D2 receptors. Nat Neurosci 16 1627 PMID: 24121738
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
Do you know of a great paper that uses Clozapine from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Dopamine Receptors Scientific Review
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
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