Clozapine structure
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Common Name | Clozapine | ||
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CAS Number | 5786-21-0 | Molecular Weight | 326.823 | |
Density | 1.3±0.1 g/cm3 | Boiling Point | 489.2±55.0 °C at 760 mmHg | |
Molecular Formula | C18H19ClN4 | Melting Point | 182-185°C | |
MSDS | Chinese USA | Flash Point | 249.6±31.5 °C | |
Symbol |
GHS06, GHS08 |
Signal Word | Danger |
Use of ClozapineClozapine (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. |
Name | clozapine |
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Synonym | More Synonyms |
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. |
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Related Catalog | |
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. |
Density | 1.3±0.1 g/cm3 |
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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 |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
MUTATION DATA
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Symbol |
GHS06, GHS08 |
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Signal Word | Danger |
Hazard Statements | H301-H341-H361 |
Precautionary Statements | Missing Phrase - N15.00950417-P280 |
Hazard Codes | Xi:Irritant |
Risk Phrases | R22;R36/37/38 |
Safety Phrases | S26 |
RIDADR | UN 2811 6.1/PG 3 |
WGK Germany | 3 |
RTECS | HP1750000 |
Packaging Group | III |
Hazard Class | 6.1(b) |
HS Code | 2933990090 |
~88% Clozapine CAS#:5786-21-0 |
Literature: Australian Journal of Chemistry, , vol. 60, # 9 p. 673 - 684 |
~41% Clozapine CAS#:5786-21-0 |
Literature: US2007/92586 A1, ; Page/Page column 13 ; |
~21% Clozapine CAS#:5786-21-0 |
Literature: US2010/166887 A1, ; US 20100166887 A1 |
~% Clozapine CAS#:5786-21-0 |
Literature: Tetrahedron, , vol. 66, # 41 p. 8203 - 8209 |
~% Clozapine CAS#:5786-21-0 |
Literature: Bioorganic and Medicinal Chemistry Letters, , vol. 16, # 17 p. 4543 - 4547 |
HS Code | 2933990090 |
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Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Antidepressants activate the lysophosphatidic acid receptor LPA(1) to induce insulin-like growth factor-I receptor transactivation, stimulation of ERK1/2 signaling and cell proliferation in CHO-K1 fibroblasts.
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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 |
5H-Dibenzo(b,e)(1,4)diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)- |
Clozapine |
Clozapine (Tautomer) |
Iprox |
8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine |
5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)- |
Clozapinum |
Azaleptine |
Clozaril |
Clozapin |
Leponex |
Fazaclo |
Lepotex |
MFCD00153785 |
8-CHLORO-11-(4-METHYL-1-PIPERAZINYL)-5H-DIBENZO(B,E)(1,4)DIA - ZEPINE |