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Nicergoline

(Synonyms: 尼麦角林)

目录号: PC10769 纯度: ≥98%

血管扩张剂,Nicergoline能抑制Alpha-1A肾上腺素受体。

CAS No. :27848-84-6

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中文名称

Nicergoline

中文别名

麦角溴烟酯;尼麦角林;10-甲氧基-1,6-二甲基麦角林-8-甲醇 5-溴烟酸酯;脑通;你先获宁;麥角溴菸鹼酯;麦角灵;Nicergoline 尼麦角林;麦角溴烟酯 EP标准品;麦角溴烟酯用于峰鉴定 EP标准品;麦角溴烟酯用于系统适应性 EP标准品;尼麦角林标准品;哌库溴铵;盐酸洛哌丁胺;[(8R,10S)-10-甲氧基-1,6-地甲基麦角林-8-基]甲基-5-溴吡啶-3-羧酸酯;5-溴吡啶-3-羧酸-[(8R,10S)-10-甲氧基-1,6-二甲基麦角林-8-基]甲酯;麦角溴烟酯麦角溴烟酯

英文名称

Nicergoline

英文别名

nicergoline;-(+)-10-methoxy-1,6-dimethylergoline-8-beta-methanol5-bromonicotinate;10-methoxy-1,6-dimethyl-ergolin-8-beta-methanol-(5-bromnicotinat);10-methoxy-1,6-dimethyl-ergoline-8-beta-methano5-bromo-3-pyridinecarboxy;10-methoxy-1,6-dimethyl-ergoline-8-beta-methano5-bromonicotinate(ester);1-methyl-lumilysergol8-(5-bromonicotinate)10-methylether;8-beta-((5-bromonicotinoyloxy)methyl)-1,6-dimethyl-10-alpha-methoxyergoline;fi6714;[(8R,10S)-10-Methoxy-1,6-dimethylergolin-8-yl]methyl 5-Bromopyridine-3-carboxylate;5-bromo-nicotinic acid 10-methoxy-1,6-dimethyl-ergolin-8-ylmethyl ester;5-Bromopyridine-3-carboxylic Acid [(8R,10S)-10-Methoxy-1,6-dimethylergolin-8-yl]methyl Ester;Cergodum;Dilasenil;Ergobel;ergoline-8-methanol 10-methoxy-1,6-dimethyl-,8-(5-bromo-3-pyridinecarboxylate);Ergotop;Memoq;mne;nargoline;nigergoline;Sermion;TA 079;5-Bromonicotinic acid 10-methoxy-1,6-dimethylergoline-8-methyl ester;Nimergoline;Nimergoline base;Nicotergoline;Nicergolinum;Nicergolin [German];Nicergolina [DCIT];Nicergolinum [INN-Latin];C24H26BrN3O3;FI 6714;RP 19651;Sermion (TN);10-Methoxy-1,6-dimethylergoline-8beta-methanol 5-bromonicotinate;JCV8365FWN;10-Methoxy-1,6-dimethylergoline-8beta-methanol 5-bromonicotinate (ester)

Cas No.

27848-84-6

分子式

C₂₄H₂₆BrN₃O₃

分子量

484.39

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

详情描述

血管扩张剂,Nicergoline能抑制Alpha-1A肾上腺素受体。

生物活性

Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α_1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimers disease.

性状

Solid

IC50 & Target[1][2]

α1A-adrenoceptor

体外研究(In Vitro)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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 Alzheimers 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	3×Tg-AD mice (male, 28-35 g, 6 weeks) with the Alzheimers 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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Alvarez-Guerra, M., N. Bertholom, and R.P. Garay, Selective blockade by nicergoline of vascular responses elicited by stimulation of alpha 1A-adrenoceptor subtype in the rat. Fundam Clin Pharmacol, 1999. 13(1): p. 50-8. [Information]

[2]. Zang G, et, al. Ameliorative effect of nicergoline on cognitive function through the PI3K/AKT signaling pathway in mouse models of Alzheimers disease. Mol Med Rep. 2018 May;17(5):7293-7300. [Information]

[3]. Mizuno T, et, al. Protective effects of nicergoline against neuronal cell death induced by activated microglia and astrocytes. Brain Res. 2005 Dec 20;1066(1-2):78-85. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (206.45 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 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。

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. Alvarez-Guerra, M., N. Bertholom, and R.P. Garay, Selective blockade by nicergoline of vascular responses elicited by stimulation of alpha 1A-adrenoceptor subtype in the rat. Fundam Clin Pharmacol, 1999. 13(1): p. 50-8. [Information]

[2]. Zang G, et, al. Ameliorative effect of nicergoline on cognitive function through the PI3K/AKT signaling pathway in mouse models of Alzheimers disease. Mol Med Rep. 2018 May;17(5):7293-7300. [Information]

[3]. Mizuno T, et, al. Protective effects of nicergoline against neuronal cell death induced by activated microglia and astrocytes. Brain Res. 2005 Dec 20;1066(1-2):78-85. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Nicergoline

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