尼麦角林
中文名称 | 尼麦角林 |
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中文同义词 | 5-溴烟酸 10-甲氧基-1,6-二甲基麦角灵-8-甲酯;麥角溴菸鹼酯;麦角溴烟酯;脑通;你先获宁;10-甲氧基-1,6-二甲基麦角林-8-甲醇 5-溴烟酸酯;尼麦角林;麦角溴烟酯用于系统适应性 EP标准品 |
英文名称 | Nicergoline |
英文同义词 | 10-methoxy-1,6-dimethyl-ergoline-8-beta-methano5-bromo-3-pyridinecarboxy;10-methoxy-1,6-dimethyl-ergoline-8-beta-methano5-bromonicotinate(ester);10-methoxy-1,6-dimethylergoline-8-methanol5-bromo-3-pyrindinecarboxylate(es;1-methyl-lumilysergol8-(5-bromonicotinate)10-methylether;8-beta-((5-bromonicotinoyloxy)methyl)-1,6-dimethyl-10-alpha-methoxyergoline;fi6714;late(ester);mne |
CAS号 | 27848-84-6 |
分子式 | C24H26BrN3O3 |
分子量 | 484.39 |
EINECS号 | 248-694-6 |
相关类别 | 小分子抑制剂;原料药;吡咯;化工原料;医药原料药-科研原料;中药对照品;Miscellaneous Natural Products;SPIROPITAN;标准品;医用原料;脑血管用药;医药原料药;杂质世界-钆布醇;脑部用药;医药原料;尼麦角林杂质;生物化工;化学试剂;Miscellaneous;Adrenoceptor |
Mol文件 | 27848-84-6.mol |
结构式 |
尼麦角林 性质
熔点 | 136-138° |
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沸点 | 594.4±50.0 °C(Predicted) |
密度 | 1.3558 (rough estimate) |
折射率 | 1.6200 (estimate) |
储存条件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 | 几乎不溶于水,易溶于二氯甲烷,溶于乙醇(96%)。 |
形态 | 固体 |
酸度系数(pKa) | 6.33±0.40(Predicted) |
颜色 | 白色至类白色 |
水溶解性 | Soluble in alcohol, chloroform, and acetone. Insoluble in water. |
Merck | 14,9496 |
未见严重不良反应的报道,少数病人可有轻微不良反应,一般为胃肠道不适(如胃痛)、面部潮红、潮热、头晕、嗜睡、失眠、低血压、耳鸣等。临床试验可观察到血液中尿酸浓度升高。
Nicergoline,溴烟碱酸的麦角林衍生物,是一种有效,选择性和具有口服活性的 α1A-肾上腺素能受体拮抗剂。Nicergoline 具有血管舒张作用。Nicergoline 可以改善阿尔茨海默症小鼠的认知功能。Target | Value |
alpha-1A adrenergic receptor
() |
Nicergoline (0.3-30 μM; 24 h) attenuates activated microglia- and astrocytes-induced neuronal cell death.
Nicergoline (0.3-30 μM; 48 h) suppresses the production of proinflammatory cytokines and superoxide anion by activated microglia.
Nicergoline (10 mg/kg; i.v. once daily for 60 d) improves impaired neurogenesis and cognitive competence in mice with Alzheimer's disease.
Nicergoline (10 mg/kg; i.v. once daily for 60 d) inhibits apoptosis, inflammation and oxidative stress in hippocampal cells, and regulates the activity of hippocampal cells through the PI3K/AKT signaling pathway in mice.
Animal Model: | 3×Tg-AD mice (male, 28-35 g, 6 weeks) with the Alzheimer's disease |
Dosage: | 10 mg/kg |
Administration: | I.v. once daily for 60 days |
Result: |
Improved neurogenesis and cognitive competence.
Decreased the degree of dementia. Downregulated pathogenic Aβ-42 and -40 peptides and APP in the hippocampi. Increased Levels of the neuroprotective forkhead box protein P2 (Foxp2), Src homology 2-containing inositol phosphatase (SxIP) and end-binding proteins (EB) in the hippocampi. Exhibited marked differences in the dispersion of the pyramidal cell layer between the nicergoline-treated and control groups. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-B0702 | Nicergoline | 5 mg | 312元 | |
2024/08/19 | HY-B0702 | 尼麦角林 Nicergoline | 27848-84-6 | 10mg | 500元 |