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Merck
CN

A7861

Sigma-Aldrich

阿塞那平马来酸盐

≥98% (HPLC)

别名:

(3aRS,12bRS)-5-Chloro-2-methyl-2,3,3a,12btetrahydro-1Hdibenzo[2,3:6,7]oxepino[4,5-c]pyrrole (2Z)-2-butenedioate, Org 5222, trans-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz(2,3:6,7)oxepino(4,5-c)pyrrole maleate

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关于此项目

经验公式（希尔记法）:
C17H16ClNO ·C4H4O4
CAS Number:
85650-56-2
分子量:
401.84
EC 号:
288-064-8
MDL编号:
MFCD00900588
UNSPSC代码:
12352200
PubChem化学物质编号:
329770943
NACRES:
NA.77

主要文件

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质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to off-white

溶解性

H2O: ≥10 mg/mL

创始人

Merck & Co., Inc., Kenilworth, NJ, U.S.

储存温度

2-8°C

SMILES字符串

OC(=O)\C=C/C(O)=O.CN1C[C@H]2[C@H](C1)c3cc(Cl)ccc3Oc4ccccc24

InChI

1S/C17H16ClNO.C4H4O4/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19;5-3(6)1-2-4(7)8/h2-8,14-15H,9-10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-,15-;/m1./s1

InChI key

GMDCDXMAFMEDAG-CHHFXETESA-N

一般描述

Asenapine maleate acts as an antimanic. It belongs to the family of dibenzoxepinopyrrolidines. Asenapine is considered to be a weak inhibitor of cytochrome P450 2D6 (CYP2D6). It increases the level of dopamine, norepinephrine and acetylcholine in brain.

应用

Asenapine maleate has been used as a stressor in studying the Fos expression in forebrain structures of rat models.
Asenapine maleate is a serotonin 5-HT and dopamine D2 receptor antagonist. Asenapine maleate can be used to treat schizophrenia and bipolar mania.

生化/生理作用

Asenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic.

特点和优势

This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

象形图

Skull and crossbonesEnvironment
GHS06,GHS09

警示用语：

Danger

危险分类

Acute Tox. 3 Oral - Aquatic Acute 1 - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

靶器官

Respiratory system

储存分类代码

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000153708
0000153709
0000153709
0000153708
0000123035

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Ahmed A Abu-Hassan et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 239, 118474-118474 (2020-05-26)
Asenapine maleate was approved by the FDA for the treatment of schizophrenia and mania or mixed episodes with bipolar I disorder. In the present article, two spectroscopic methods were developed and validated for the determination of asenapine. Both methods depend
Frank I Tarazi et al.
Drugs of today (Barcelona, Spain : 1998), 45(12), 865-876 (2010-02-06)
Schizophrenia and bipolar disorder are serious neuropsychiatric disorders with substantial health risks for patients that result in major socioeconomic burdens on society. Current therapeutic agents fail to adequately address patient needs in terms of efficacy, tolerability and treatment-related adverse events.
The preclinical profile of asenapine: clinical relevance for the treatment of schizophrenia and bipolar mania
Tarazi FI and Neill JC
Expert Opinion on Drug Discovery, 8(1), 93-103 (2013)
Jakub Trawiński et al.
Ecotoxicology and environmental safety, 162, 272-286 (2018-07-11)
The photolytic and photocatalytic transformation of an antipsychotic drug asenapine with the use of H2O2 and TiO2 was studied. A method employing irradiation with a simulated full solar spectrum in the photostability chamber was applied, then the reverse-phase ultra high
Juilee A Kulkarni et al.
Current drug delivery, 15(4), 520-531 (2017-11-23)
Asenapine is an anti-psychotic agent approved by the US-FDA for treatment of acute schizophrenia and manic or bipolar I disorder in adults. It is poorly absorbed when administered orally, hence exhibits poor oral bioavailability, which limits its use in clinical
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