| CAS |
5786-21-0 |
| Chinese Name |
氯氮平 |
| English Name |
Clozapine |
| Synonyms |
HF 1854;LX 100-129 |
| Molecular Formula |
C18H19ClN4 |
| Molecular Weight |
326.83 |
| Solubility |
Soluble in DMSO ≥10mg/mL |
| Purity |
HPLC≥98% |
| Appearance |
Light yellow to yellow Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 227-313-7 |
| MDL |
MFCD00153785 |
| SMILES |
CN1CCN(CC1)C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42 |
| Target Point |
5-HT2;Dopamine Receptor;mAChR |
| Passage |
Neuronal Signaling;GPCR & G Protein |
| Background |
Clozapine is an effective antagonist of the dopamine receptor and an agonist of the selective muscarinic M4 receptor. Clozapine inhibits muscarinic M1 receptor and 5HT2A receptor. Clozapine can be used in research related to schizophrenia. |
| Biological Activity |
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 |
5-HT2A Receptor:4nM(Ki，Inhibitor);mAChR1:9.5nM(Ki，Antagonist);mAChR4:11nM(EC50，Agonist);α2-adrenergic receptor:51nM(Ki，Inhibitor);D2 Receptor:75nM(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]. |
| 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]. |
| Animal Experiment |
Animal Model[3]: Male 129 S6/Sv mice，lysergic acid diethylamide(LSD)-induced psychosis model;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. |
| Data Literature Source |
[1]. Seeman P，et al. Clozapine，a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9.
[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.
[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.
[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. |
| Unit |
Piece |
| Specification |
100mg 10mM*1mL in DMSO 200mg 500mg |
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