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阿塞那平马来酸盐 /Asenapine maleate {[allProObj[0].p_purity_real_show]}

货号:A504366 同义名: 阿塞那平盐酸盐 / Org 5222 maleate;Org 5222

Asenapine Maleate is a 5-HT and dopamine D2 receptor antagonist used to treat schizophrenia and bipolar mania.

Asenapine maleate 化学结构 CAS号:85650-56-2
Asenapine maleate 化学结构
CAS号:85650-56-2
Asenapine maleate 3D分子结构
CAS号:85650-56-2
Asenapine maleate 化学结构 CAS号:85650-56-2
Asenapine maleate 3D分子结构 CAS号:85650-56-2
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Asenapine maleate 纯度/质量文件 产品仅供科研

货号:A504366 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

98%
Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

98%
Venlafaxine 98%
Fluvoxamine maleate 99%
Iloperidone 98%
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 97%
Trazodone 98+%
Clomipramine HCl 98%
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

97%
Duloxetine 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 98%
Fluoxetine HCl 99.5%
Paroxetine hydrochloride AChR 97%
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

98%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

99%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

98%
Tropisetron 99%
Palonosetron 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

98%
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron hydrochloride dihydrate 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

98%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

99%+
Intepirdine ++++

5-HT6, pKi: 9.63

99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Asenapine maleate 生物活性

靶点
  • α-adrenergic receptor

    α2A-adrenergic receptor, pKi:8.9

    α2B-adrenergic receptor, pKi:8.9

  • 5-HT2

    5-HT2C, pKi:10.46

    5-HT2A, pKi:9.75

  • 5-HT6

    5-HT6, pKi:9.6

  • 5-HT1

    5-HT1A, pKi:8.6

    5-HT1B, pKi:8.4

描述 Asenapine maleate is an antagonist of 5-HT (1a, 1b, 2a, 2b, 2C, 5A, 6, 7) and D2, with Ki values of 0.03-4.0 nm and 1.3 nm, respectively and also an antipsychotic[3]. Asenapine reduced freezing behaviour and increased serotonin release in the rat hippocampus[4]. Asenapine ameliorated this serotonin deficit in a dose-related manner that matched its efficacy for reversing the cognitive deficit[5].In vivo, Asenapine displays robust antimanic property and effective antagonistic activity at 5‐HT 1A/7 receptors[6].

Asenapine maleate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02181803 Schizophrenia Phase 1 Completed - -
NCT02600741 - Completed - -
NCT03565068 Schizophrenia Phase 1 Suspended(Study is on hold pen... 展开 >>ding evaluation of emerging preclinical findings) 收起 << October 9, 2019 United States, California ... 展开 >> California Clinical Trials ( Site 0001) Glendale, California, United States, 91206 收起 <<

Asenapine maleate 参考文献

[1]Stoner SC, Pace HA. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40.

[2]Shahid M, Walker GB, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73.

[3]Shahid M, Walker GB, Zorn SH, Wong EH. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. PMID: 18308814.

[4]Ohyama M, Kondo M, Yamauchi M, Imanishi T, Koyama T. Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Acta Neuropsychiatr. 2016 Dec;28(6):327-336. doi: 10.1017/neu.2016.17. Epub 2016 Apr 21. PMID: 27099073.

[5]Elsworth JD, Groman SM, Jentsch JD, Valles R, Shahid M, Wong E, Marston H, Roth RH. Asenapine effects on cognitive and monoamine dysfunction elicited by subchronic phencyclidine administration. Neuropharmacology. 2012 Mar;62(3):1442-52. doi: 10.1016/j.neuropharm.2011.08.026. Epub 2011 Aug 23. PMID: 21875607; PMCID: PMC3711239.

[6]Delcourte S, Abrial E, Etiévant A, Rovera R, Arnt J, Didriksen M, Haddjeri N. Asenapine modulates mood-related behaviors and 5-HT1A/7 receptors-mediated neurotransmission. CNS Neurosci Ther. 2017 Jun;23(6):518-525. doi: 10.1111/cns.12698. Epub 2017 Apr 17. PMID: 28417559; PMCID: PMC6492759.

Asenapine maleate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.44mL

2.49mL

1.24mL

24.89mL

4.98mL

2.49mL

Asenapine maleate 技术信息

CAS号85650-56-2
分子式C21H20ClNO5
分子量 401.84
别名 阿塞那平盐酸盐 ;Org 5222 maleate;Org 5222
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 25 mg/mL(62.21 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 6 mg/mL(14.93 mM)

动物实验配方
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