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Blonanserin

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Company Name: Capot Chemical Co.,Ltd.
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Products Intro: Product Name:2-(4-Ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
CAS:132810-10-7
Purity:98%(Min,HPLC) Package:100g;1kg;5kg,10kg,25kg,50kg
Company Name: Linyi Shengxin Pharmaceutical R&D Co., Ltd  Gold
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Products Intro:Product Name:Blonanserin
CAS:132810-10-7
Purity:99% HPLC Package:10g;100g;1kg
Company Name: Zhuhai Yourun Co., Ltd.  Gold
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Products Intro:Product Name:Blonanserin
CAS:132810-10-7
Purity:99% HPLC Package:5KG;1KG
Company Name: Shanghai Boyle Chemical Co., Ltd.  
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Products Intro:Product Name:CYCLOOCTABPYRIDINE, 2-(4-ETHYL-1-PIPERAZINYL)-4-(4-FLUOROPHENYL)-5,6,7,8,9,10-HEXAHYDRO-
CAS:132810-10-7
Company Name: SiChuang NanBu Honesty Technology Co., Ltd.  
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Products Intro:CAS:132810-10-7
Purity:>=99.5%
Blonanserin Basic information
Outline Synthesis method Atypical antipsychotic drugs China Patent Information Uses
Product Name:Blonanserin
Synonyms:CYCLOOCTA[B]PYRIDINE, 2-(4-ETHYL-1-PIPERAZINYL)-4-(4-FLUOROPHENYL)-5,6,7,8,9,10-HEXAHYDRO-;Blonanserin;AD 5423;2-(4-Ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine;2-(4-Ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine;Lonasen;Blonansarin –;Blonanserin, AD-5423, Lonasen
CAS:132810-10-7
MF:C23H30FN3
MW:367.5028032
EINECS:
Product Categories:APIs;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals
Mol File:132810-10-7.mol
Blonanserin Structure
Blonanserin Chemical Properties
Melting point 117-119°C
storage temp. Refrigerator
solubility DMSO: ≥10mg/mL
color white to off-white
Safety Information
Hazard Codes Xn
Risk Statements 22
RTECS GY0175140
MSDS Information
Blonanserin Usage And Synthesis
OutlineThis product is a serotonin and dopamine antagonist (SDA), it is a second-generation atypical antipsychotic drugs, and has a considerable dopamine D2 receptor blocking action as haloperidol , it also has a strong 5-HT2A blocking effect, the selectivity on both receptors is stronger than other antipsychotics. It displays fewer extrapyramidal response side effects than conventional antipsychotics on the market . It is developed and sold by Sumitomo Pharmaceutical Co., Ltd. of Japan. Listing: April 2008 in Japan.
Synthesis methodFluorobenzoate condensates with acetonitrile to get fluorobenzoyl acetonitrile, prepared in polyphosphoric acid by the reaction of 3-(4-fluorophenyl)-3-oxo-propionamide, and cyclooctanone cyclization of 4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cyclooctane and [b] pyridin-2 (1H)-one, and recrystallized from benzene dichloride Lin acid dichloride with N-ethylpiperazine nucleophilic substitution to give antipsychotic blonanserin, the overall yield is about 42%.
Author: Junfang Wang, Xiaomei Wang , Zhefeng Wang , Huilin Shi
Author unit: Shanghai Institute of Pharmaceutical Industry
Journal Name: Chinese Journal of Pharmaceuticals 2009 40 (4)
Atypical antipsychotic drugsSchizophrenia is a common psychiatric disease, since the early 1950s, for the discovery of antipsychotic effects of chiorpromazinum. Schizophrenia has been treated with drugs.
According to receptor blocking actions, the commonly used antipsychotics are divided into two categories, naming the typical and atypical: typical antipsychotics are represented by chlorpromazine and haloperidol . The main mechanism is blocking dopamine receptors, it has a good effect on positive symptoms of schizophrenia (hallucinations, delusions, agitation, impulsive behavior, etc.) . Meanwhile extrapyramidal effects (EPS) are common, while the effects for negative symptoms (apathy, poverty of thought, will decline, etc.) are poor, while atypical antipsychotics show a wider spectrum for the treatment of negative symptoms better than traditional medicine, and it is safe, with more mild side effects, the dosage is smaller, there have been many more advanced forms, which greatly improve patient compliance, representative drugs include clozapine, risperidone, olanzapine .
Double-blind clinical trials for 8 weeks for blonanserin comparison with haloperidol shown, 263 patients with schizophrenia were involved. 8-24mg/day blonanserin is at least effective as 4-12mg/day of haloperidol, it can improve the final grade improvement rate(FGIR) score (at least two drugs in patients with moderate improvement rate of 61.2% and 51.3%, respectively), less incidence of extrapyramidal side effects (52.7% and 75.4%).
The above information is edited by the chemicalbook of Tian Ye.
China Patent InformationJanuary 2008 blonanserin was developed and sold by Sumitomo Pharmaceutical Co., Ltd. of Japan. This product was compound patent in 1989 . The patent has expired.
At present, the domestic product is not imported, according to the "Patent Law" and "Regulations on Administrative Protection Drugs" , the drug patent risk does not exist in China, it does not have the conditions of application for administrative protection.
UsesMental
Chemical PropertiesPale Yellow Solid
UsesBlonanserin is a novel atypical antipsychotic agent with potent dopamine D2 (Ki, 14.8 nM) and serotonin 5-HT2(Ki, 3.98 nM) receptors antagonist properties.
UsesA 5-HT2 Serotonin receptor and D2 Dopamine receptor antagonist, used as an antipsychotic.
Blonanserin Preparation Products And Raw materials
Tag:Blonanserin(132810-10-7) Related Product Information
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