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

Clozapine  (Synonyms: HF 1854)

Cat. No.: HY-14539 Purity: 99.99%
COA Handling Instructions

Clozapine (HF 1854) 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.

Clozapine Chemical Structure

Clozapine Chemical Structure

CAS No. : 5786-21-0

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Based on 2 publication(s) in Google Scholar

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Description

Clozapine (HF 1854) 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[1][4]

5-HT2A Receptor

4 nM (Ki, Inhibitor)

5-HT6 Receptor

 

5-HT7 Receptor

 

mAChR1

9.5 nM (Ki, Antagonist)

mAChR4

11 nM (EC50, Agonist)

α2-adrenergic receptor

51 nM (Ki, Inhibitor)

D2 Receptor

75 nM (Ki, Antagonist)

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].

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

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.
Clinical Trial
Molecular Weight

326.82

Appearance

Solid

Formula

C18H19ClN4
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (152.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0598 mL 15.2989 mL 30.5979 mL
5 mM 0.6120 mL 3.0598 mL 6.1196 mL
10 mM 0.3060 mL 1.5299 mL 3.0598 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.65 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.65 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.65 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Keywords:

Clozapine5786-21-0HF 1854HF1854HF-1854Dopamine ReceptormAChRAdrenergic Receptor5-HT ReceptorMuscarinic acetylcholine receptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorantipsychoticschizophreniaHeLapsychosisInhibitorinhibitorinhibit

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