Clozapine dihydrochloride
Based on 13 publication(s) in Google Scholar
Clozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
For research use only. We do not sell to patients.
- CAS No.: 2711603-38-0
- Formula: C18H21Cl3N4
- Molecular Weight:399.75
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Publications Citing Use of MedChemExpress (MCE) Clozapine dihydrochloride
More- Nat Commun. 2026 Jun 16. [Abstract]
- Nat Commun. 2025 Dec 13;16(1):11318. [Abstract]
- Nat Commun. 2024 Sep 1;15(1):7603. [Abstract]
- Mol Psychiatry. 2021 Jun;26(6):2514-2532. [Abstract]
- Commun Med (Lond). 2025 Jul 1;5(1):249. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Int J Mol Sci. 2026 Apr 9;27(8):3381. [Abstract]
- Eur J Pharm Sci. 2023 Aug 1:187:106475. [Abstract]
- Eur J Pharm Sci. 2021 Sep 1:164:105889. [Abstract]
- FEBS J. 2024 Nov;291(21):4680-4695. [Abstract]
- Biochem Biophys Res Commun. 2025 Oct 30:786:152756. [Abstract]
- bioRxiv. 2024 November 03.
- bioRxiv. 2024 Jun 8:2024.06.07.597973. [Abstract]
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All Dopamine Receptor Isoforms
MoreAll Adrenergic Receptor Isoforms
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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5-HT2A Receptor |
5-HT2A Receptor 4 nM (Ki) |
5-HT6 Receptor |
5-HT7 Receptor |
mAChR1 9.5 nM (Ki) |
mAChR4 11 nM (EC50) |
α2-adrenergic receptor 51 nM (Ki) |
D2 Receptor 75 nM (Ki) |
Clozapine (HF 1854) is a D2 receptor antagonist with a Ki of 75 nM, blocks the serotonin 5HT2A receptor with a Ki of 4 nM, inhibits the muscarinic M1 receptor with a Ki of 9.5 nM, blocks α2-adrenoceptor with a Ki value of 51 nM[1].
Clozapine (0-1 μM; 24 h) downregulates 5-HT6 and upregulates 5-HT7 receptors in HeLa cells[2].
Clozapine is a full agonist at the muscarinic M4 receptor (EC50=11 nM) expressed in CHO cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male 129 S6/Sv mice, lysergic acid diethylamide (LSD)-induced psychosis model[3].
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Dosage:25 mg/kg/day.
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Administration:Intraperitoneal injection, 21 days.
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Result:Decreased head-twitch response, reduced 5-HT2A mRNA, rescued induction of c-fos, but not egr-1 and egr-2.
Chemical Information
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CAS No. 2711603-38-0
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Molecular Weight 399.75
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Formula C18H21Cl3N4
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SMILES
CN1CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42)CC1.Cl.Cl
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Synonyms
HF 1854 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
Targeting dopamine transporter for treating social transmission of depression-like behaviors in male mice. [Abstract]2026 Jun 16. PMID: 42303982 -
Nat Commun
Norepinephrine-mediated arousal fluctuations drive inverted U-shaped functional connectivity dynamics. [Abstract]2025 Dec 13;16(1):11318. PMID: 41390822
Clozapine dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Dec 13;16(1):11318. [Abstract]
In isoflurane anesthetized mice, the injection of Clozapine (0.03 mg/kg; i.p.) significantly increased EEG-based arousal index, but from a low to middle arousal level.
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Nat Commun
2024 Sep 1;15(1):7603. PMID: 39217143
Clozapine dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 1;15(1):7603. [Abstract]
Representative current clamp recording of a NPYDRN/vlPAG-hM4Di neuron with the bath of Clozapine (5 μM). Average membrane potential and firing frequency before and after Clozapine application to inhibit NPY DRN/vlPAGneurons were also recorded. Clozapine effectively inhibited hM4Di+ NPYDRN/vlPAG neurons with decreased neuronal membrane potential and firing frequency.
Clozapine dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 1;15(1):7603. [Abstract]
Percentage of body weight changes, daily food intake and its area under curve (AUC) of mCherry-restraint and hM4Di-restraint mice. Clozapine (i.p.; 0.2mg/kg; 30 min before restraint for 14 d) caused NPYhM4Di mice to consume less food and lost more body weight than NPYmCherry mice during chronic restraint stress.
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Mol Psychiatry
2021 Jun;26(6):2514-2532. PMID: 33303946
Clozapine dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2021 Jun;26(6):2514-2532. [Abstract]
The administration of Clozapine (i.p.; 2 d) restored impaired PPI in female ZFP804A mutant mice.
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Commun Med (Lond)
AI-enabled drug prediction and gene network analysis reveal therapeutic use of vorinostat for Rett Syndrome in preclinical models. [Abstract]2025 Jul 1;5(1):249. PMID: 40595330 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Int J Mol Sci
A Clozapine-Responsive GPCR-Based Gene Switch for Pharmacological Control of Gene Expression in Mammalian Cells and In Vivo. [Abstract]2026 Apr 9;27(8):3381. PMID: 42074026 -
Eur J Pharm Sci
Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes. [Abstract]2023 Aug 1:187:106475. PMID: 37225005 -
Eur J Pharm Sci
Atypical kinetics of cytochrome P450 2J2: Epoxidation of arachidonic acid and reversible inhibition by xenobiotic inhibitors. [Abstract]2021 Sep 1:164:105889. PMID: 34044117 -
FEBS J
TRPM7 controls skin keratinocyte senescence by targeting intracellular calcium signaling. [Abstract]2024 Nov;291(21):4680-4695. PMID: 39185948
Clozapine dihydrochloride purchased from MedChemExpress. Usage Cited in: FEBS J. 2024 Nov;291(21):4680-4695. [Abstract]
HaCaT cells were transfected with siNC or siRNA against TRPM7 and then treated with Clozapine (Clo) (10 μM; 6 d) the next day. Clozapine (Clo) promoted activation of TRPM7 and increased SA-b-Gal activity.
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Biochem Biophys Res Commun
Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]2025 Oct 30:786:152756. PMID: 41043280 -
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bioRxiv
Functional coupling between MC4R and Kir7.1 contributes to clozapine-induced hyperphagia. [Abstract]2024 Jun 8:2024.06.07.597973. PMID: 38895206
Purity & Documentation
References
[1]. Seeman P, et al. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9. [Content Brief]
[2]. Zhukovskaya NL, et al. Clozapine downregulates 5-hydroxytryptamine6 (5-HT6) and upregulates 5-HT7 receptors in HeLa cells. Neurosci Lett. 2000 Jul 21;288(3):236-40. [Content Brief]
[3]. Moreno JL, et al. Persistent effects of chronic clozapine on the cellular and behavioral responses to LSD in mice. Psychopharmacology (Berl). 2013 Jan;225(1):217-26. [Content Brief]
[4]. Zorn SH, et al. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Clozapine dihydrochloride Related Classifications
HY-14539B Related Classifications
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