2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor
  4. Clozapine dihydrochloride

Clozapine dihydrochloride  (Synonyms: HF 1854 dihydrochloride)

Cat. No.: HY-14539B
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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

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Clozapine dihydrochloride Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    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.

    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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    Description

    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[1][2][3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[4].

    IC50 & Target

    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)

    In Vitro

    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.

    Clozapine dihydrochloride Related Antibodies
    In Vivo

    Clozapine (HF 1854) (25 mg/kg/day; i.p.; 21 days) shows antipsychotic effects in lysergic acid diethylamide-induced psychosis mouse model[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male 129 S6/Sv mice, lysergic acid diethylamide (LSD)-induced psychosis model[3].
    Dosage: 25 mg/kg/day.
    Administration: Intraperitoneal injection, 21 days.
    Result: Decreased head-twitch response, reduced 5-HT2A mRNA, rescued induction of c-fos, but not egr-1 and egr-2.
    Molecular Weight

    399.75

    Formula

    C18H21Cl3N4
    CAS No.
    SMILES

    CN1CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42)CC1.Cl.Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    Clozapine dihydrochloride Related Classifications

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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Clozapine2711603-38-0HF 1854HF1854HF-1854Dopamine ReceptormAChRAdrenergic Receptor5-HT ReceptorMuscarinic acetylcholine receptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorantipsychoticschizophreniaHeLapsychosisInhibitorinhibitorinhibit

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