Brexpiprazoleimpuritya
Brexpiprazole
CAS: 913611-97-9
Molecular Formula: C25H27N3O2S
Brexpiprazoleimpuritya - Names and Identifiers
Brexpiprazoleimpuritya - Physico-chemical Properties
| Molecular Formula | C25H27N3O2S |
| Molar Mass | 433.57 |
| Density | 1.245±0.06 g/cm3(Predicted) |
| Melting Point | 179 - 181oC |
| Boling Point | 675.2±55.0 °C(Predicted) |
| Solubility | DMSO: ≥ 48 mg/mL |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 11.22±0.70(Predicted) |
| Storage Condition | Refrigerator |
| Physical and Chemical Properties | Bioactive Brexpiprazole(OPC-34712) is a new type of dopamine receptor D2 and serotonin 1A receptor partial agonist, and is also an antagonist of serotonin 2A receptor, norepinephrine alpha1B and alpha2C receptor. Its Ki values for D2L,5-HT1A,5-HT2A,α1B receptor and α2C receptor were 0.3,0.12,0.47,0.17 and 0.59nM, respectively. |
| Use | Application of epizole can be used for major depression, schizophrenia adjuvant therapy medication. |
| In vitro study | Brexpiperazole is a potent partial activator of human serotonin 5-HT1A(Ki = 0.12 nM) and dopamine receptor D2L(Ki = 0.3 nM). It is also an antagonist of the 5-HT2A receptor (Ki = 0.47 nM). It also has antagonistic activity against human norepinephrine receptors α1B(Ki = 0.17 nM) and α2C(Ki = 0.59 nM). In addition, brexpiperazole has moderate affinity for human D3, 5-HT2B, 5-HT7, α1A and α1D adrenergic receptors. In PC12 cells, it enhances NGF-induced neurite outgrowth and enhances the effect of fluoxetine on neurite outgrowth. |
| In vivo study | Brexpiperazole can improve PCP-191 caused by Cognitive Disorder in mice through the 5-HT1A receptor. |
Brexpiprazoleimpuritya - Pharmacological effects and clinical evaluation of the 5-hydroxytryptamine-dopamine receptor partial agonist epipimazole
From VIP
Author:
Xu lei ,< a href = "https://xueshu.baidu.com/usercenter/data/author?cmd=authoruri&wd=authoruri:(f6dcfc07c756858c) author:(Feng Yufei)" target = "_blank"> Feng Yufei
Summary:
Ipiperazole is a new type of partial agonist that mainly acts on dopamine D2 receptors. In addition, it also has 5-HT1A partial receptor agonism, α1-adrenal receptor antagonism and 5-HT2A partial receptor antagonism. It is mainly used for adjuvant treatment of schizophrenia and major depression (MDD). The most common adverse reactions of this product are akathisia, weight gain and anxiety. This article reviews the pharmacological effects, pharmacokinetics, clinical evaluation, safety, usage and dosage, and drug interactions of epipprazole through literature retrieval.
keywords:
epipimazole schizophrenia major depression 5-hydroxytryptamine-dopamine receptor partial agonist pharmacological action clinical evaluation
cited:
Year:
2016
Last Update：2024-01-02 23:10:35
Brexpiprazoleimpuritya - A method for the synthesis of epipimazole
From Titanium Academic
Inventor:
Wang Yusheng ,< a href = "https://xueshu.baidu.com/s?wd=author: (Jiao Yinglu) & tn = SE_baiduxueshu_c1gjeupa & ie = utf-8 & SC _f_para = SC _hilight = person" target = "_blank"> Jiao Yinglu ,< a href = "https://xueshu.baidu.com/s?wd=author: (Wang Boyu) & tn = SE_baiduxueshu_c1gjeupa & ie = utf-8 & SC _f_para = SC _hilight = person" target = "_blank"> Wang Boyu , Huang Luning , gu hong
Summary:
The purpose of the present invention is to provide a new synthesis method of epipizole (Brexpiprazole):(a) using the compound of formula I or its salt as raw material and compound A under alkaline conditions in an aprotic solvent by halogenation reaction to obtain intermediate II;(B) The intermediate II is reacted with compound III, that is, the obtained epipizole is compound IV, the reaction formula is as follows: wherein: compound A is halogenated butane, X1 and X2 are halogens, selected from chlorine or bromine; X1 and X2 can be the same or different halogens.
Last Update：2023-08-16 22:23:51
Brexpiprazoleimpuritya - Technology to improve the solubility of epipizole and the preparation method of tablets Technical field
from Baidu library
patent type:
patent for invention
application (patent) number:
CN201910896974.5
date of application:
20190923
public/announcement number:
CN112535669A
date of publication/announcement:
20210323
Applicant (patentee):
Beijing wanquan dezhong pharmaceutical biotechnology co., ltd
Inventor:
national and provincial code:
CN110114
Summary:
The present invention relates to a technology for improving the solubility of the insoluble drug ipiperazole and the preparation of ipiperazole tablets, belonging to the technical field of pharmaceutical preparations. Epiprazole is used as the active ingredient of the drug for airflow crushing, and then hydrophilic excipients are used to make solid dispersion, which can ensure the highly dispersed state of the drug, effectively improve the solubility and dissolution rate of the insoluble drug, thereby improving the bioavailability of the drug. Then the solid dispersion is further prepared into tablets to promote the absorption of the drug in the body, and further improve the bioavailability of the drug, and its preparation process is simple, avoiding dust pollution, easy industrial production, and enhancing the compliance of patients with medication.
Last Update：2023-08-16 22:23:51
Brexpiprazoleimpuritya - Preparation method of epipprazole
from Baidu library
Application (Patent) No.:
CN 201510934582
Applicant (patentee):
Nanjing Edkaiteng Biomedical Co., Ltd.
Inventor:
Wang Xuegen , he lingyun , Yu Yang , Jin Haojie , Guo liqin
cited:
Summary:
The present invention belongs to the technical field of chemical drug synthesis, and specifically relates to a preparation method of epipizole. The method prepares crystalline epipizole through a five-step method. The method has the advantages of high synthesis yield, simple operation, easy purification and stable final product. In addition, the present invention effectively avoids the use of metal catalysts, and at the same time greatly reduces the reaction steps, thereby reducing the difficulty of the reaction, thereby simplifying the post-treatment, improving the yield and greatly reducing the reaction cost, which is beneficial to industrial production.
Last Update：2023-08-16 22:23:51
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Brexpiprazoleimpuritya
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