Chemical Name: 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
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).
Deuterated analog also available.
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.
DA receptor pharmacology.
Seeman and Van Tol
Trends Pharmacol.Sci., 1994;15:264
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.
Binding of typical and atypical antipsychotics to 5-HT1C and 5-HT2 sites: cloz. potently interacts with 5-HT1C sites.
Canton et al.
The involvement of DA D1 and D2 receptors in the effects of the classical neuroleptic halope. and the atypical neuroleptic cloz.
Ellenbroek et al.
Citations for Clozapine
The citations listed below are publications that use Tocris products. Selected citations for Clozapine include:
18 Citations: Showing 1 - 10
Identifying the In Vivo Cellular Correlates of Antipsychotic Drugs.
Authors: Joshi and Panicker
5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.
Authors: Peng Et al.
Disrupted-in-schizophrenia1 (DISC1) L100P mutation alters synaptic transmission and plasticity in the hippocampus and causes recognition memory deficits.
Authors: Cui Et al.
Mol Brain 2016;9:89
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
Chronic Antipsychotic Treatment in the Rat - Effects on Brain Interleukin-8 and Kynurenic Acid.
Authors: Larsson Et al.
Brain Res 2015;8:49
Curcumin Mitigates the Intracellular Lipid Deposit Induced by Antipsychotics In Vitro.
Authors: Canfrán-Duque Et al.
Int J Tryptophan Res 2015;10:e0141829
Pramipexole reduces phosphorylation of α-synuclein at serine-129.
Authors: Chau Et al.
Exp Mol Med 2013;51:573
Age-dependent regulation of synaptic connections by DA D2 receptors.
Authors: Jia Et al.
Nat Neurosci 2013;16:1627
D4 DA receptors modulate NR2B NMDA receptors and LTP in stratum oriens of hippocampal CA1.
Authors: Herwerth Et al.
Cereb Cortex 2012;22:1786
HDAC2 regulates atypical antipsychotic responses through the modulation of mGlu2 promoter activity.
Authors: Kurita Et al.
Nat Neurosci 2012;15:1245
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
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
Activation of the JAK-STAT pathway is necessary for desensitization of 5-HT2A receptor-stimulated phospholipase C signalling by olanzapine, cloz. and MDL 100907.
Authors: Singh Et al.
Int J Neuropsychopharmacol 2009;12:651
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
Differential regulation of central BDNF protein levels by antidepressant and non-antidepressant drug treatments.
Authors: Balu Et al.
J Mol Neurosci 2008;1211:37
Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs.
Authors: Hampson Et al.
Haloperidol and cloz. differentially regulate signals upstream of glycogen synthase kinase 3 in the rat frontal cortex.
Authors: Roh Et al.
Front Cell Neurosci 2007;39:353
N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-MthD.-aspartate receptor activity.
Authors: Sur Et al.
Proc Natl Acad Sci U S A 2003;100:13674
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