Clozapine
Clozapine is an atypical antipsychotic medication [1]
Clozapine has been considered an atypical antipsychotic medication because of their therapeutic efficacy in the treatment of schizophrenic patients resistant to conventional neuroleptics. In addition, Clozapine has shown the effect on binding 5HT1c and 5HT2 sites with pKi values of 8.07 and 7.63, respectively. Besides, Clozapine has been reported to recognize all human dopamine receptor subtypes with Ki values of 80nM, 230nM, 89nM, 141nM and 250nM for D2, D3, D4, D1 and D5 receptor, respectively. Clozapine has been found to be the only drug to have a higher affinity for 5-HT1c sites than for the 5-HT2, D1 and D2 receptors [1].
References:
[1] Canton H1, Verrièle L, Colpaert FC. Binding of typical and atypical antipsychotics to 5-HT1C and 5-HT2 sites: clozapine potently interacts with 5-HT1C sites. Eur J Pharmacol. 1990 Nov 20; 191(1):93-6.
| Storage | Store at -20°C |
| M.Wt | 326.82 |
| Cas No. | 5786-21-0 |
| Formula | C18H19ClN4 |
| Solubility | insoluble in H2O; ≥14.95 mg/mL in DMSO; ≥2.7 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 3-chloro-6-(4-methylpiperazin-1-yl)-5H-benzo[b][1,4]benzodiazepine |
| SDF | Download SDF |
| Canonical SMILES | CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment: | |
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Cell lines |
Prefrontal cortical (PFC) neurons, Rats hepatocytes |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1-10 μM for 16-72 h; or 20 - 80 μM for 48 h |
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Applications |
Clozapine induced initial pERK1-specific blockade and subsequent activation of the ERK response in prefrontal cortical (PFC) neurons in vitro [1]. Moreover, Clozapine (20-80 μM) concentration-dependently induced hepatotoxicity [2]. |
| Animal experiment: | |
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Animal models |
C57BL/6 mouse model, Male Sprague-Dawley (SD) rats model |
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Dosage form |
1, 2.5 mg/kg; intraperitoneal administration, for 15 h, 24 h; or 25 mg/kg, oral administration, for 7 days |
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Applications |
Clozapine induced ERK1/2 cell signaling activation via the EGF receptor in mouse prefrontal cortex [1]. Moreover, Clozapine treatment led to marked accumulation of triglyceride and increase in gglutamyl transpeptidase (g-GT) activity, liver weight, and serum AST in rats [2]. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Pereira, A., Sugiharto-Winarno, A., Zhang, B., Malcolm, P., Fink, G. and Sundram, S. (2012) Clozapine induction of ERK1/2 cell signalling via the EGF receptor in mouse prefrontal cortex and striatum is distinct from other antipsychotic drugs. Int J Neuropsychopharmacol. 15, 1149-1160 2. Jia, L. L., Zhong, Z. Y., Li, F., Ling, Z. L., Chen, Y., Zhao, W. M., Li, Y., Jiang, S. W., Xu, P., Yang, Y., Hu, M. Y., Liu, L. and Liu, X. D. (2014) Aggravation of clozapine-induced hepatotoxicity by glycyrrhetinic acid in rats. J Pharmacol Sci. 124, 468-479 |
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