Home
Clozapine

Clozapine

Catalog No.

B2235

5-HT receptor antagonist

Skip to the beginning of the images gallery

Grouped product items
Size	Price	Stock	Qty
10mM (in 1mL DMSO)	$55.00	In stock
1g	$52.00	In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background
Product Citation
Chemical Properties
Protocol
Quality Control

Background

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.

Product Citation

1. Anderson AG, Gaffy CB, et al. "Inhibition of Epstein-Barr Virus Lytic Reactivation by the Atypical Antipsychotic Drug Clozapine." Viruses. 2019 May 17;11(5). pii: E450. PMID:31108875

Chemical Properties

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.

Protocol

Cell experiment:
Cell lines	Prefrontal cortical (PFC) neurons, Rats hepatocytes
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.
Reacting condition	0.1-10 μM for 16-72 h; or 20 - 80 μM for 48 h
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:
Animal models	C57BL/6 mouse model, Male Sprague-Dawley (SD) rats model
Dosage form	1, 2.5 mg/kg; intraperitoneal administration, for 15 h, 24 h; or 25 mg/kg, oral administration, for 7 days
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].
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.
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