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54241-01-9

54241-01-9 Structure

54241-01-9 Structure
IdentificationBack Directory
[Name]

5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)-, hydrochloride (1:1)
[CAS]

54241-01-9
[Synonyms]

5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)-, hydrochloride (1:1)
[Molecular Formula]

C18H20Cl2N4
[MOL File]

54241-01-9.mol
[Molecular Weight]

363.29
Chemical PropertiesBack Directory
[form ]

solid
[color ]

Orange
[Water Solubility ]

Soluble in water (100 mM). Always store solutions at -20°C.
Hazard InformationBack Directory
[Uses]

Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively[1][2][3]. Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[4].
[in vivo]

Clozapine hydrochloride (25 mg/kg/day; i.p.; 21 days) shows antipsychotic effects in lysergic acid diethylamide-induced psychosis mouse model[3].

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.
[IC 50]

5-HT2A Receptor: 4 nM (Ki); 5-HT6 Receptor; Human 5-HT7 Receptor; mAChR1: 9.5 nM (Ki); mAChR4: 11 nM (EC50); α2-adrenergic receptor: 51 nM (Ki); D2 Receptor: 75 nM (Ki)
[storage]

-20°C
[References]

[1] Seeman P, et al. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9. DOI:10.1021/cn400189s
[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. DOI:10.1016/s0304-3940(00)01225-8
[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. DOI:10.1007/s00213-012-2809-7
[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. DOI:10.1016/0922-4106(94)90047-7
54241-01-9 suppliers list
Company Name: TargetMol Chemicals Inc.
Tel: +8613564774135 , +8613564774135
Website:
Company Name: TargetMol Chemicals Inc.  
Tel: 15002134094
Website: https://www.targetmol.cn/
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