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。
| 生物活性 | Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist ofα1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease[1][2]. |
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体外研究
(In Vitro) | Nicergoline (0.3-30 μM; 24 h) attenuates activated microglia- and astrocytes-induced neuronal cell death[3].
Nicergoline (0.3-30 μM; 48 h) suppresses the production of proinflammatory cytokines and superoxide anion by activated microglia[3].
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体内研究
(In Vivo) | Nicergoline (10 mg/kg; i.v. once daily for 60 d) improves impaired neurogenesis and cognitive competence in mice with Alzheimer's disease[2].
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[2].
| Animal Model: | 3×Tg-AD mice (male, 28-35 g, 6 weeks) with the Alzheimer's disease[2] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(206.45 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.0645 mL | 10.3223 mL | 20.6445 mL | | 5 mM | 0.4129 mL | 2.0645 mL | 4.1289 mL | | 10 mM | 0.2064 mL | 1.0322 mL | 2.0645 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制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 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.16 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.16 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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