 
        
        
        
                货号:A504366
                
                同义名:
                    
                        
                            阿塞那平盐酸盐
                            
                             / Org 5222 maleate; Org 5222
                            
                        
                    
                
                
                
                    
                     
                    
                     
                
            
Asenapine maleate 是一种高亲和性 5-HT 和 D2 受体拮抗剂(Ki 分别为 0.03–4.0 nM 和 1.3 nM),并具有多种 5-HT 受体亚型拮抗作用,适用于精神分裂症和双相情感障碍等精神疾病模型的研究。
 
                                 
                                
                            

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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 | ✔ | 99% | |||||||||||||||||
| Fluvoxamine maleate | ✔ | 99% | |||||||||||||||||
| Iloperidone | ✔ | 99% | |||||||||||||||||
| 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 | ✔ | 97% | |||||||||||||||||
| Sertraline HCl | ++ 5-HT, Ki: 13 nM | 98% | |||||||||||||||||
| Citalopram HBr | +++ serotonin reuptake, IC50: 1.8 nM | 98% | |||||||||||||||||
| Latrepirdine 2HCl | ✔ | GluR | 99% | ||||||||||||||||
| Fluoxetine HCl | ✔ | 99.5% | |||||||||||||||||
| Paroxetine HCl | ✔ | AChR | 99% | ||||||||||||||||
| 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 | 95% | ||||||||||||||||
| LY310762 | + 5-HT1D, Ki: 249 nM | 99%+ | |||||||||||||||||
| Cyclobenzaprine HCI | ✔ | 99% | |||||||||||||||||
| Blonanserin | +++ 5-HT2, Ki: 3.98 nM | 99% | |||||||||||||||||
| 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 | 98% | |||||||||||||||||
| Agomelatine | ✔ | 98% | |||||||||||||||||
| Clozapine | ✔ | 98% | |||||||||||||||||
| Amitriptyline | + 5-HT2, Ki: 235 nM | SERT | 99% | ||||||||||||||||
| PRX-08066 maleate | +++ 5-HT2B, IC50: 3.4 nM | 98+% | |||||||||||||||||
| RS-127445 | ++++ 5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5 | 99%+ | |||||||||||||||||
| Sarpogrelate HCl | ++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM | 98% | |||||||||||||||||
| Tropisetron | ✔ | 99% | |||||||||||||||||
| Ramosetron HCl | ++++ 5-HT3 receptor, Ki: 0.091 nM | 98% | |||||||||||||||||
| Ondansetron | ✔ | 99% | |||||||||||||||||
| Granisetron | ✔ | 98% | |||||||||||||||||
| Alosetron HCl | ✔ | 98% | |||||||||||||||||
| Ondansetron HCl dihydrate | ✔ | 98% | |||||||||||||||||
| VUF10166 | ++++ 5-HT3AB, Ki: 22 nM 5-HT3A, Ki: 0.04 nM | 99%+ | |||||||||||||||||
| Azasetron HCl | ++++ 5-HT3, IC50: 0.33 nM | 99% | |||||||||||||||||
| Asenapine maleate | +++ 5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6 | ++++ 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-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2 | + 5-HT6, pKi: 5.9 | + 5-HT7, pKi: 6.3 | 95% | ||||||||||||||
| 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。 | |||||||||||||||||||
| 靶点 | 
 | 
| 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]. | 
| 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 << | 
| 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 | |
| CAS号 | 85650-56-2 | 
| 分子式 | C21H20ClNO5 | 
| 分子量 | 401.84 | 
| SMILES Code | CN1C[C@]2([H])C3=CC=CC=C3OC4=CC=C(Cl)C=C4[C@]2(C1)[H].O=C(O)/C=C\C(O)=O | 
| MDL No. | MFCD00900588 | 
| 别名 | 阿塞那平盐酸盐 ;Org 5222 maleate; Org 5222 | 
| 运输 | 蓝冰 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C | 
| 溶解方案 | 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) 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
 
 
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