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Brexpiprazole (OPC-34712) 是人5-HT1A 和多巴胺受体的部分激动剂,Ki 分别为0.12 和 0.3 nM。它也是5-HT2A 受体的拮抗剂,Ki 为 0.47 nM,可作为非典型抗精神病药。

Brexpiprazole (OPC-34712) 是人5-HT1A 和多巴胺受体的部分激动剂,Ki 分别为0.12 和 0.3 nM。它也是5-HT2A 受体的拮抗剂,Ki 为 0.47 nM,可作为非典型抗精神病药。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 156 | In stock | |
| 5 mg | ¥ 338 | In stock | |
| 10 mg | ¥ 479 | In stock | |
| 25 mg | ¥ 689 | In stock | |
| 50 mg | ¥ 892 | In stock | |
| 100 mg | ¥ 1,280 | In stock | |
| 200 mg | ¥ 1,990 | In stock |
Brexpiprazole 相关产品
| 产品描述 | Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors. |
| 靶点活性 | D2L:0.3 nM(Ki), 5-HT1A:0.12 nM(Ki), α2C-adrenoceptor:0.59 nM(Ki), Noradrenaline α1B (human):0.17 nM(Ki), 5-HT2A receptor:0.47 nM(Ki) |
| 体外活性 | Brexpiprazole是一种在人体5-羟色胺 (5-HT) 5-HT1A (Ki=0.12 nM) 和多巴胺D2L (Ki=0.3 nM) 受体上表现出强有力部分激动剂活性,并在5-HT2A受体上表现出拮抗活性 (Ki=0.47 nM) 的化合物。它同样在人体去甲肾上腺素α1B (Ki=0.17 nM) 和α2C受体 (Ki=0.59 nM) 上显示出强有力的拮抗作用。此外,该化合物对人体D3、5-HT2B和5-HT7受体,以及α1A和α1D肾上腺素受体表现出中等亲和力。Brexpiprazole增强了PC12细胞中NGF诱导的神经突生长。它可以显着增强fluoxetine(或paroxetine)对神经突生长的效果[1]。 |
| 体内活性 | Brexpiprazole可通过5-HT1A受体减轻PCP-191在小鼠中引起的认知缺失[2]。 |
| 细胞实验 | 2.5 ng/ml of NGF(nerve growth factor) is used to study the potentiating effects of brexpiprazole on neurite outgrowth. Twenty-four hours after plating, the medium is replaced with DMEM medium containing 0.5% FBS and 1% penicillin-streptomycin with NGF (2.5 ng/ml), with or without brexpiprazole (0.001, 0.01, 0.1 or 1.0 μM). Four days after incubation with NGF (2.5 ng/ml) with or without drugs, morphometric analysis is performed on digitized images of live cells taken under phase-contrast illumination, with an inverted microscope linked to a camera. (Only for Reference) |
| 别名 | 依匹唑派, 依匹哌唑, OPC-34712 |
| 分子量 | 433.57 |
| 分子式 | C25H27N3O2S |
| CAS No. | 913611-97-9 |
| Smiles | C(CCCOC=1C=C2C(=CC1)C=CC(=O)N2)N3CCN(C4=C5C(SC=C5)=CC=C4)CC3 |
| 密度 | 1.245 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| 溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 4.34 mg/mL (10 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||
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