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Submit ReviewClozapine
说明： Dopamine antagonist with some D4 selectivity; also 5-HT2A/2C antagonist
化学名： 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
纯度： ≥99% (HPLC)
生物活性 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).
技术数据 for Clozapine
| 分子量 | 326.83 |
| 公式 | C18H19ClN4 |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Clozapine
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 32.68 | 100 | |
| 2eq.HCl | 16.34 | 50 温和加热 |
制备储备液 for Clozapine
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Clozapine
参考文献 for Clozapine
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for Clozapine, please let us know.
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关键词: 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 篇 Clozapine 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Clozapine 的部分引用包括：
Dong et al (2020) A projection from the paraventricular nucleus of the thalamus to the shell of the nucleus accumbens contributes to footshock stress-induced social avoidance Neurobiol Stress 13 PMID: 33344719
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
Maldonado et al (2021) Oxytocin shapes spontaneous activity patterns in the developing visual cortex by activating somatostatin interneurons. Curr Biol 31 322 PMID: 33157028
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
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
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
Joshi and Panicker (2019) Identifying the In Vivo Cellular Correlates of Antipsychotic Drugs. Eneuro 5 PMID: 30713996
Peng et al (2018) 5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology. Cell 172 719 PMID: 29398112
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
Chau et al (2013) Pramipexole reduces phosphorylation of α-synuclein at serine-129. Exp Mol Med 51 573 PMID: 23681749
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
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
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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.