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/ 多巴胺受体 / Clozapine/氯氮平

Clozapine/氯氮平 {[allProObj[0].p_purity_real_show]}

货号：A592547 同义名： HF 1854; LX 100-129

Clozapine 是一种多巴胺及其他受体拮抗剂，对 M1 受体 Ki 为 9.5 nM，常用于精神分裂症的研究。

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Type HazMat fee for 500 gram (Estimated)
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Clozapine/氯氮平 化学结构 CAS号：5786-21-0
Clozapine/氯氮平 化学结构
CAS号：5786-21-0
Clozapine/氯氮平 3D分子结构
CAS号：5786-21-0
Clozapine/氯氮平 化学结构 CAS号：5786-21-0
Clozapine/氯氮平 3D分子结构 CAS号：5786-21-0
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Clozapine/氯氮平 纯度/质量文件 产品仅供科研

货号：A592547 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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产品名称 D1 receptor ↓ D2 receptor ↓ D3 receptor ↓ D4 receptor ↓ D5 receptor ↓ DAT ↓ Dopamine receptor ↓ 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

 		98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

 		99%
Tetrahydroberberine +

D2 receptor, pKi: 6.08

 		98+%
Prochlorperazine Maleate ✔ 98% (HPLC)
Olanzapine ✔ 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

 		98%
Ropinirole HCl ++

D2 receptor, Ki: 29 nM

 		99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

 		98%
Levosulpiride ✔ 99+%
Pridopidine ✔ 95%
Metoclopramide ✔ ✔ 99+%
Molindone HCl ✔ 99%
Sulpiride ✔ 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

 		99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

 		99%
Phenothiazine ✔ 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

 		+++

Dopamine D2 receptor, Ki: 3.0 nM

 		++++

Dopamine D3 receptor, Ki: 0.83 nM

 		98%
Rotundine ++

D1 receptor, IC50: 166 nM

 		+

D2 receptor, IC50: 1.47 μM

 		+

D3 receptor, IC50: 3.25 μM

 		98%
Domperidone ✔ 99+%
ONC206 ✔ 99%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

 		+++

Dopamine D2 Receptor, pKi: 8.19

 		++

Dopamine D4.4 Receptor, pKi: 7.54

 		97%
Loxapine succinate ++

D2 receptor (Human), Ki: 62 nM

D1 receptor (human), Ki: 26 nM

 		++

D2 receptor (human), Ki: 24 nM

D2 receptor (bovine), Ki: 26 nM

 		+++

D4 receptor (human), Ki: 7.5 nM

 		98%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

 		+++

D2 receptor, Ki: 2.96 nM

 		+++

D3 receptor, Ki: 4.56 nM

 		+++

D5 receptor, Ki: 9 nM

 		99%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

 		++++

D5 dopamine receptor, Ki: 0.3 nM

 		98%
MPP+ iodide ✔ 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

 		97%
Benztropine mesylate ++

DAT, IC50: 118 nM

 		98%
Azaperone ✔ 98%
Ziprasidone HCl ✔ 98+%
Paliperidone ✔ 98%
Alizapride HCl ✔ 99+%
Amisulpride ✔ 98%
Quetiapine hemifumarate ✔ Adrenergic Receptor 98%
Clozapine N-oxide ✔ 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Clozapine/氯氮平 生物活性

靶点

  • 5-HT2
描述 Clozapine was a full agonist at the muscarinic M4 receptor (EC50 = 11 nM), producing inhibition of forskolin-stimulated cAMP accumulation. In contrast, clozapine potently antagonized agonist-induced responses at the other four muscarinic receptor subtypes[3]. The chemical structure of clozapine facilitates a relatively rapid dissociation from D2 receptors. Clozapine is very potent at D2 receptor with a Ki of 75 nM. Clozapine is also potent at the α2-adrenoceptor with a Ki value of 51 nM[4]. Mice were treated chronically (21 days) with 25 mg/kg/day clozapine. Head-twitch response was decreased and [(3)H]ketanserin binding was downregulated in 1, 7, and 14 days after chronic clozapine. 5-HT ( 2A ) mRNA was reduced 1 day after chronic clozapine[5]. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine can lower the seizure threshold in a dose- and time-dependent manner. Careful patient selection and monitoring are required when clozapine therapy is used in patients with schizophrenia[6].

Clozapine/氯氮平 细胞实验

Cell Line
Concentration Treated Time Description References
NT2-N cells 10 µM 24 h Clozapine upregulated ribosomal gene expression but downregulated protein synthesis. Int J Mol Sci. 2022 Jun 28;23(13):7180.
microglial cells 10 μM 24 h To evaluate the effect of Clozapine on poly (I:C)-induced inflammatory cytokines, results showed that Clozapine significantly reduced the levels of IL-1α, IL-1β, IL-2, and IL-17. Cells. 2020 Feb 28;9(3):577.
HEK293 cells 10 μM overnight To investigate the effect of Clozapine on mGluR2 density and subcellular localization, results showed that Clozapine reduced mGluR2 density and subcellular colocalization through 5-HT2AR-mGluR2 heteromerization. Sci Signal. 2020 Oct 20;13(654):eaaw3122.
SH-SY5Y cells 1μM 24 h To evaluate the protective effect of Clozapine-N-Oxide (CNO) on rotenone-induced toxicity in SH-SY5Y cells. Results showed that CNO dose-dependently restored the cell viability of rotenone-treated SH-SY5Y cells, with 0.01μM CNO showing high efficacy in reducing rotenone-induced neurotoxicity. Free Radic Biol Med. 2024 Feb 20;212:384-402.
Primary astrocytes 20 μM or 40 μM 24 h To evaluate the effect of Clozapine on CCL2 and CCL5 mRNA expression in activated astrocytes. Results showed that Clozapine treatment had no significant effect on the expression of CCL2 or CCL5 mRNA in activated astrocytes. J Neuroinflammation. 2020 Feb 12;17(1):53.
Bone marrow-derived macrophages (BMMO) 20 μM or 40 μM 24 h To evaluate the effect of Clozapine on CCL2 and CCL5 mRNA expression in activated macrophages. Results showed that Clozapine treatment significantly reduced the expression of CCL2 and CCL5 mRNA in activated macrophages. J Neuroinflammation. 2020 Feb 12;17(1):53.
Primary microglia 20 μM 24 h To evaluate the effect of Clozapine on CCL2 and CCL5 mRNA expression in activated microglia. Results showed that Clozapine pre-treatment or co-treatment significantly reduced LPS-induced CCL2 mRNA expression, while CCL5 mRNA was only significantly reduced by co-treatment. J Neuroinflammation. 2020 Feb 12;17(1):53.
Primary astrocytes 20 μM or 40 μM 24 h To evaluate the effect of Clozapine on CCL2 and CCL5 mRNA expression. Results showed that Clozapine treatment had no significant effect on CCL2 or CCL5 mRNA expression in astrocytes. J Neuroinflammation. 2020 Feb 12;17(1):53.
Bone marrow-derived macrophages (BMMO) 20 μM or 40 μM 24 h To evaluate the effect of Clozapine on CCL2 and CCL5 mRNA expression. Results showed that Clozapine treatment reduced the expression of CCL2 and CCL5 mRNA in activated macrophages. J Neuroinflammation. 2020 Feb 12;17(1):53.
Primary microglia 20 μM 24 h To evaluate the effect of Clozapine on CCL2 and CCL5 mRNA expression. Results showed that Clozapine pre-treatment or co-treatment reduced LPS-induced CCL2 and CCL5 mRNA expression. J Neuroinflammation. 2020 Feb 12;17(1):53.
HL60 cells 2.5–20 µM 8, 24, or 48 h Analyzed the effects of clozapine on metabolic fluxes, cell respiration, and intracellular ATP. Results showed that clozapine reduced Akt activation via neuroreceptor inhibition, decreased glucose uptake, and induced ER stress and the unfolded protein response (UPR). Metabolic profiling revealed downregulation of glycolysis and the pentose phosphate pathway, while upregulation of F0F1-ATPase inhibitory factor 1 (IF1) led to a 30–40% reduction in oxygen consumption in HL60 cells. Cells. 2024 Apr 29;13(9):762.

Clozapine/氯氮平 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Rotenone-induced Parkinson's disease model Subcutaneous injection 1mg/kg Twice daily for 3 weeks To evaluate the protective effects of CNO and CLZ on rotenone-induced motor deficits and dopaminergic neurodegeneration. Results showed that CNO and CLZ significantly ameliorated rotenone-induced motor deficits and dopaminergic neuron degeneration, while NDC showed only partial protective effects. Free Radic Biol Med. 2024 Feb 20;212:384-402.
Female C57BL/6 mice Experimental autoimmune encephalomyelitis (EAE) Oral (via drinking water) 60 mg/kg Starting one day before immunization and continuing throughout the experiment To evaluate the effect of Clozapine on immune cell infiltration and disease severity in the EAE model. Results showed that Clozapine treatment significantly reduced the infiltration of monocytes, neutrophils, and T cells into the CNS and decreased the expression of CCL2 and CCL5 mRNA in the brain and spinal cord. J Neuroinflammation. 2020 Feb 12;17(1):53.
Mice Wild-type mice Intraperitoneal injection 1, 5, and 10 mg/kg Single injection, observed for 6 hours To test the effects of CNO on sleep, found a dose-dependent suppression of REM sleep, changes in EEG spectral power during NREM sleep, and altered sleep architecture Elife. 2023 Mar 9;12:e84740
C57BL/6 J mice Experimental autoimmune encephalomyelitis (EAE) Drinking water 60 mg/kg Starting one day before immunization and continuing throughout the experiment To evaluate the effect of Clozapine on immune cell infiltration and disease severity in the EAE model. Results showed that Clozapine reduced the infiltration of peripheral immune cells into the CNS and decreased the expression of CCL2 and CCL5 transcripts in the brain and spinal cord. J Neuroinflammation. 2020 Feb 12;17(1):53.
Mice PnocIRES-Cre mice Intraperitoneal injection 3 mg/kg 30 minutes before Inhibition of PnocCeA neurons reduced high-fat diet intake Neuron. 2019 Jun 5;102(5):1037-1052.e7
Mice Trigeminal neuralgia model Intraperitoneal injection 2.5 mg/kg Single administration Inhibition of LHb neuronal activity by chemicogenetic methods alleviated pT-ION-induced anxiety-like behaviors Acta Neuropathol Commun. 2020 Apr 7;8(1):44
Mice Wild-type mice Intraperitoneal injection 0.1 mg/kg Single dose To investigate the effects of Clozapine on NAc activation, results showed that Clozapine activation of NAc induced positive affect and suppressed intruder-induced hyperthermia and PGE2-induced fever. iScience. 2024 Oct 18;27(11):111197
Rhesus monkeys Pathological anxiety model Intramuscular injection 0.03 mg/kg or 0.1 mg/kg Single administration, 30 minutes before behavioral testing To assess the effects of low-dose clozapine on anxiety-related behaviors, results showed that clozapine selectively decreased anxiety-related freezing behavior in the human intruder paradigm in hM4Di-expressing monkeys, while coo vocalizations and locomotion were unaffected Mol Ther. 2021 Dec 1;29(12):3484-3497

Clozapine/氯氮平 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00031317 Panic Disorder Phase 4 Completed - United States, Maryland ... 展开 >> National Institute of Mental Health (NIMH) Bethesda, Maryland, United States, 20892 收起 <<
NCT02949752 Antipsychotics Weight Gain Phase 4 Recruiting August 2017 Singapore ... 展开 >> Institute of Mental Health Recruiting Singapore, Singapore, 556121 Contact: Bee Choo Lim    63892000 ext 3618    Bee_Choo_LIM@imh.com.sg    Contact: Jaclyn Ong    63892000 ext 2959    jaclyn_yy_ong@imh.com.sg 收起 <<
NCT02926976 Schizophrenia Not Applicable Recruiting September 2018 China ... 展开 >> DTliu Recruiting Shanghai, China Contact: DT Liu, PHD       erliu110@126.com 收起 <<

Clozapine/氯氮平 参考文献

[1]Seeman P. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9.

[2]Nguyen TV, Kosofsky BE, et al. Differential expression of c-fos and zif268 in rat striatum after haloperidol, clozapine, and amphetamine. Proc Natl Acad Sci U S A. 1992 May 15;89(10):4270-4.

[3]Zorn SH, Jones SB, Ward KM, Liston DR. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2

[4]Seeman P. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9

[5]Moreno JL, Holloway T, Umali A, Rayannavar V, Sealfon SC, González-Maeso J. Persistent effects of chronic clozapine on the cellular and behavioral responses to LSD in mice. Psychopharmacology (Berl). 2013 Jan;225(1):217-26

[6]Jann MW, Grimsley SR, Gray EC, Chang WH. Pharmacokinetics and pharmacodynamics of clozapine. Clin Pharmacokinet. 1993 Feb;24(2):161-76

Clozapine/氯氮平 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.06mL

0.61mL

0.31mL

15.30mL

3.06mL

1.53mL

30.60mL

6.12mL

3.06mL

Clozapine/氯氮平 技术信息

CAS号5786-21-0
分子式C18H19ClN4
分子量 326.82
SMILES Code CN1CCN(CC1)C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42
MDL No. MFCD00153785
别名 HF 1854; LX 100-129; Clozapine (CRM)
运输蓝冰
InChI Key QZUDBNBUXVUHMW-UHFFFAOYSA-N
Pubchem ID 135398737
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

DMSO: 50 mg/mL(152.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Clozapine | 5786-21-0 | HF 1854 | HF1854 | HF-1854 | Dopamine Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Dopamine Receptor | mAChR | Adrenergic Receptor | 5-HT Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Clozapine/氯氮平 纯度/质量文件 | Clozapine/氯氮平 亚型比较 | Clozapine/氯氮平 生物活性 | Clozapine/氯氮平 临床数据 | Clozapine/氯氮平 参考文献 | Clozapine/氯氮平 实验方案 | Clozapine/氯氮平 技术信息

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