Clozapine (Synonyms: HF 1854) |
| Catalog No.GC17760 |
Clozapine(HF 1854)은 정신분열증 연구에 사용되는 항정신병약물입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 5786-21-0
Sample solution is provided at 25 µL, 10mM.
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Clozapine (HF 1854) is an antipsychotic used to treat schizophrenia. Clozapine is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for M1 receptor[1][2][3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[4].
Clozapine shows the unique property of having antipsychotic action but no Parkinson-like motor side effects. The chemical structure of clozapine facilitates a relatively rapid dissociation from D2 receptors. After short-term occupation of D2 receptors, peak neural activity raises synaptic dopamine, which then displaces clozapine. While clozapine also occupies other types of receptors, they may not have a significant role in preventing parkinsonism. Clozapine is very potent at D2 receptor with a Ki of 75 nM. Clozapine is also potent at the α2-adrenoceptor with a Ki value of 51 nM[1]. Clozapine causes paradoxical downregulation of 5-HT2A receptors. Clozapine also binds to 5-HT6 and 5-HT7 receptors with high affnity[2].
Head-twitch response is decreased and [3H]ketanserin binding is downregulated in 1, 7, and 14 days after chronic clozapine. 5-HT2A mRNA is reduced 1 day after chronic clozapine. Induction of c-fos, but not egr-1 and egr-2, is rescued 7 days after chronicclozapine[3].
References:
[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.
| 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. |
|
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 |
|
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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| Cas No. | 5786-21-0 | SDF | |
| Synonyms | HF 1854 | ||
| Chemical Name | 3-chloro-6-(4-methylpiperazin-1-yl)-5H-benzo[b][1,4]benzodiazepine | ||
| Canonical SMILES | CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl | ||
| Formula | C18H19ClN4 | M.Wt | 326.82 |
| Solubility | ≥ 14.95mg/mL in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0598 mL | 15.2989 mL | 30.5979 mL |
| 5 mM | 612 μL | 3.0598 mL | 6.1196 mL |
| 10 mM | 306 μL | 1.5299 mL | 3.0598 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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