尼麥角林
| 中文名稱 | 尼麥角林 |
|---|---|
| 中文同義詞 | 5-溴煙酸 10-甲氧基-1,6-二甲基麥角靈-8-甲酯;麥角溴菸鹼酯;麥角溴煙酯;腦通;你先獲寧;10-甲氧基-1,6-二甲基麥角林-8-甲醇 5-溴煙酸酯;尼麥角林;麥角溴煙酯用于系統(tǒng)適應(yīng)性 EP標(biāo)準(zhǔn)品 |
| 英文名稱 | Nicergoline |
| 英文同義詞 | 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號(hào) | 27848-84-6 |
| 分子式 | C24H26BrN3O3 |
| 分子量 | 484.39 |
| EINECS號(hào) | 248-694-6 |
| 相關(guān)類別 | 小分子抑制劑;原料藥;吡咯;化工原料;醫(yī)藥原料藥-科研原料;標(biāo)準(zhǔn)品;醫(yī)用原料;中藥對(duì)照品;腦血管用藥;醫(yī)藥原料藥;雜質(zhì)世界-釓布醇;腦部用藥;醫(yī)藥原料;尼麥角林雜質(zhì);生物化工;Miscellaneous Natural Products;Miscellaneous;Adrenoceptor;SPIROPITAN;化學(xué)試劑 |
| Mol文件 | 27848-84-6.mol |
| 結(jié)構(gòu)式 |  |
尼麥角林 性質(zhì)
| 熔點(diǎn) | 136-138° |
|---|---|
| 沸點(diǎn) | 594.4±50.0 °C(Predicted) |
| 密度 | 1.3558 (rough estimate) |
| 折射率 | 1.6200 (estimate) |
| 儲(chǔ)存條件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| 溶解度 | 幾乎不溶于水，易溶于二氯甲烷，溶于乙醇（96%）。 |
| 形態(tài) | 固體 |
| 酸度系數(shù)(pKa) | 6.33±0.40(Predicted) |
| 顏色 | 白色至類白色 |
| 水溶解性 | Soluble in alcohol, chloroform, and acetone. Insoluble in water. |
| Merck | 14,9496 |
未見嚴(yán)重不良反應(yīng)的報(bào)道，少數(shù)病人可有輕微不良反應(yīng)，一般為胃腸道不適（如胃痛）、面部潮紅、潮熱、頭暈、嗜睡、失眠、低血壓、耳鳴等。臨床試驗(yàn)可觀察到血液中尿酸濃度升高。
Nicergoline，溴煙堿酸的麥角林衍生物，是一種有效，選擇性和具有口服活性的 α1A-腎上腺素能受體拮抗劑。Nicergoline 具有血管舒張作用。Nicergoline 可以改善阿爾茨海默癥小鼠的認(rèn)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 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2025/05/22 | HY-B0702 | 尼麥角林 Nicergoline | 27848-84-6 | 5 mg | 312元 |
| 2025/05/22 | HY-B0702 | 尼麥角林 Nicergoline | 27848-84-6 | 10mg | 500元 |