Nuciferine - CAS:475-83-2

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Nuciferine (Synonyms:荷叶碱)

目录号 : KM13971 CAS No. : 475-83-2 纯度 : 98%

Data Sheet 产品使用指南

Nuciferine 是一种 5-HT_2A，5-HT_2C 和 5-HT_2B 拮抗剂，IC₅₀ 分别为 478 nM，131 nM 和 1 μM；也是 5-HT₇ 的反向激动剂，IC₅₀ 为 150 nM。

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5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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生物活性

Nuciferine is an antagonist at 5-HT_2A (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

体外研究

Nuciferine is a partial agonist at DD₂ receptor with an activity (E_max=67% of dopamine) similar to aripiprazole (E_max=50% of dopamine). In line with its partial agonist activity, Nuciferine inhibited dopamine-induced activation of G_i with a potency similar to clozapine (Nuciferine K_B=62 nM; Clozapine K_B=20 nM) as determined via Schild regression analysis. The natural product Nuciferine acts as an effective inhibitor of adult worm motility. Nuciferine is effective at inhibiting both basal and 5-HT evoked motility of adult schistosomes. Nuciferine inhibits Sm.5HTR_L and schistosomule with 0.24±0.04 and 0.62±0.22 μM, respectively.

体内研究

In rodent models relevant to antipsychotic drug action, Nuciferine blocks head-twitch responses and discriminative stimulus effects of a 5-HT_2A agonist, substituted for clozapine discriminative stimulus, enhanced amphetamine induced locomotor activity, inhibited phencyclidine (PCP)-induced locomotor activity, and rescued PCP-induced disruption of prepulse inhibition without induction of catalepsy. In the presence of 1 or 3 mg/kg Nuciferine, cumulative PCP doses produce similar substitution to PCP alone. In the clozapine-trained animals, a dose-dependent substitution for 1.25 mg/kg clozapine is seen at 10 mg/kg Nuciferine (80.63% drug lever responding), with an ED₅₀ value of 5.42 mg/kg (95% CI 3.09-9.48 mg/kg) while the lower doses tested (0.1 mg/kg-3 mg/kg) fails to produce substitution for clozapine’s discriminative cue. In addition to a high percentage of responding on the clozapine-appropriate lever, 10 mg/kg Nuciferine also produces significant rate suppression as compared to vehicle control points (p<0.001).

分子式

C₁₉H₂₁NO₂

分子量

295.38

CAS号

475-83-2

中文名称

荷叶碱

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

溶解性数据

In Vitro:

DMSO : 11.11 mg/mL (37.61 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3855 mL	16.9273 mL	33.8547 mL
5 mM	0.6771 mL	3.3855 mL	6.7709 mL
10 mM	0.3385 mL	1.6927 mL	3.3855 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在 6 个月内使用，-20°C 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: ≥ 1.11 mg/mL (3.76 mM); Clear solution

此方案可获得 ≥ 1.11 mg/mL (3.76 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 11.1 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: ≥ 1.11 mg/mL (3.76 mM); Clear solution

此方案可获得 ≥ 1.11 mg/mL (3.76 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 11.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。