尼普拉嗪
| 中文名称 | 尼普拉嗪 |
|---|---|
| 中文同义词 | 尼普拉嗪;N-(4-(4-(4-氟苯基)哌嗪-1-基)丁-2-基)烟酰胺 |
| 英文名称 | Niaprazine |
| 英文同义词 | Niaprazine;1709 CERM;N-[3-[4-(4-Fluorophenyl)-1-piperazinyl]-1-methylpropyl]nicotinamide;N-[3-[4-(p-Fluorophenyl)-1-piperazinyl]-1-methylpropyl]nicotinamide;N-[3-[4-(4-Fluorophenyl)-1-piperazinyl]-1-methylpropyl]-3-pyridinecarboxamide;Nopron;N-(4-(4-(4-FLUOROPHENYL)PIPERAZIN-1-YL)BUTAN-2-YL)NICOTINAMIDE;3-Pyridinecarboxamide, N-[3-[4-(4-fluorophenyl)-1-piperazinyl]-1-methylpropyl]- |
| CAS号 | 27367-90-4 |
| 分子式 | C20H25FN4O |
| 分子量 | 356.4371032 |
| EINECS号 | 2484315 |
| 相关类别 | |
| Mol文件 | 27367-90-4.mol |
| 结构式 |  |
尼普拉嗪 性质
| 熔点 | 131℃ |
|---|---|
| 密度 | 1.165 |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：100 mg/mL（280.55 mM） |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
Niaprazine 是一种具有强效镇静作用的组胺 H1 受体 (histamine H1-receptor) 拮抗剂。Niaprazine 具有抗组胺和抗血清素活性，并可用于睡眠障碍的研究。
Niaprazine exhibits a low affinity for the vesicular monoamine transporter and for D2, α2, β, H1 and mAch receptors. Niaprazine, particularly the (+)stereoisomer, has a higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, but is poorly recognized by 5-HT1A and 5-HT1B binding sites.
Niaprazine (60 mg/kg; i.p.; once) treatment increases rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. Niaprazine also produces a short-lasting depletion of rat brain noradrenaline (NA) and dopamine (DA).
| Animal Model: | Male Sprague-Dawley rats (150-200 g) |
| Dosage: | 60 mg/kg |
| Administration: | Intraperitoneal injection; once |
| Result: | Increased rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. |
安全信息
| 毒性 | LD50 in mice (mg/kg): 890 orally, 145 i.v. (Mauvernay) |
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/11/08 | HY-105542 | 尼普拉嗪 Niaprazine | 27367-90-4 | 5mg | 500元 |
| 2024/11/08 | HY-105542 | Niaprazine | 10 mM * 1 mLin DMSO | 550元 |