CAS Number5786-21-0
Synonyms8-Chloro-11-(4-methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine; Asaleptin; 3-chloro-6-(4-methylpiperazin-1-yl)-5H-benzo[b][1,4]benzodiazepine; EINECS 227-313-7; 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[h,e][1,4]diazepine; 8-chloro-11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine; Clorazil; Clozapine; Clozapine (Tautomer); Iprox; 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine; Clozapinum; Azaleptine; Clozaril; Clozapin; Leponex; Fazaclo; Lepotex; MFCD00153785; 8-CHLORO-11-(4-METHYL-1-PIPERAZINYL)-5H-DIBENZO(B,E)(1,4)DIA - ZEPINE
Molecular FormulaC18H19ClN4
Molecular Weight326.82
Purity98.00%
Density1.3±0.1 g/cm3
Boiling Point489.2±55.0 °C at 760 mmHg
Melting Point182-185°C
Appearancepowder
Symbol
Signal WordWarning
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 5786-21-0 |
| Catalog No. | 2A-9032171 |
| Chinese Name | 氯氮平 |
| Synonyms | 8-Chloro-11-(4-methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine; Asaleptin; 3-chloro-6-(4-methylpiperazin-1-yl)-5H-benzo[b][1,4]benzodiazepine; EINECS 227-313-7; 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[h,e][1,4]diazepine; 8-chloro-11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine; Clorazil; Clozapine; Clozapine (Tautomer); Iprox; 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine; Clozapinum; Azaleptine; Clozaril; Clozapin; Leponex; Fazaclo; Lepotex; MFCD00153785; 8-CHLORO-11-(4-METHYL-1-PIPERAZINYL)-5H-DIBENZO(B,E)(1,4)DIA - ZEPINE |
| Molecular Formula | C18H19ClN4 |
| Molecular Weight | 326.82 |
| Purity | 98.00 |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 489.2±55.0 °C at 760 mmHg |
| Melting Point | 182-185°C |
| Appearance | powder |
| Water Solubility | ethanol: 1 mg/mL |
| Storage Condition | Store at room temperature, away from light, in a c |
| Packaging | III |
| Application | Clozapine (HF 1854) is an antipsychotic drug used to treat schizophrenia. Clozapine is a potent antagonist of dopamine and many other receptors, binding to the M1 receptor with a Ki of 9.5 nM. |
| HTC | 2933990090 |
| PubChem ID | 24277892 |
| MDL Number | MFCD00153785 |
| SMILES | CN1CCN(CC1)C2=Nc3cc(Cl)ccc3Nc4ccccc24 |
| InChI | 1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3 |
| InChI Key | QZUDBNBUXVUHMW-UHFFFAOYSA-N |
| NACRES Code | NA.77 |
| UNSPSC | 12352200 |
| Hazard Symbols | 6.1(b) |
| MSDS | msds/32171_1_5786_21_0.pdf |
| Bioactivity | 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. Related Catalog Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease Target Ki: 9.5 nM (M1), 51 nM (α2-adrenoceptor), 75 nM (D2)[1] In Vitro 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]. In Vivo 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]. Animal Admin Mice: Mice are treated chronically (21 days) with 25 mg/kg/day clozapine. Experiments are conducted 1, 7, 14, and 21 days after the last clozapine administration. [3H]Ketanserin binding and 5-HT2A mRNA expression are determined in mouse somatosensory cortex. Head-twitch behavior, expression of c-fos, which is induced by all 5-HT2A agonists, and expression of egr-1 and egr-2, which are LSD-like specific, are assayed[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. Chemical & Physical Properties Density 1.3±0.1 g/cm3 Boiling Point 489.2±55.0 °C at 760 mmHg Melting Point 182-185°C Molecular Formula C18H19ClN4 Molecular Weight 326.823 Flash Point 249.6±31.5 °C Exact Mass 326.129822 PSA 30.87000 LogP 2.36 Vapour Pressure 0.0±1.2 mmHg at 25°C Index of Refraction 1.681 Storage condition Store at RT Water Solubility ethanol: 1 mg/mL |
| Use of | 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. Properties Articles129 Name clozapine Synonym More Synonyms Clozapine Biological Activity Description 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. Related Catalog Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease Ki: 9.5 nM (M1), 51 nM (α2-adrenoceptor), 75 nM (D2)[1] In Vivo 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. Chemical & Physical Properties Exact Mass 326.129822 PSA 30.87000 Index of Refraction 1.681 Storage condition Store at RT |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Purity: 98.0% |
| MSDS Transport Info | Module 14. Shipping information United Nations classification: Item 1 Poisons. UN number: 2811 Proper Shipping Name: Toxic Solid, Organic, Not Otherwise Specified Packing grade: III |
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