Nuciferine is an antagonist at5-HT_2A(IC₅₀=478 nM),5-HT_2C(IC₅₀=131 nM), and5-HT_2B(IC₅₀=1 μM), an inverse agonist at5-HT₇(IC₅₀=150 nM), a partial agonist atD₂(EC₅₀=64 nM),D₅(EC₅₀=2.6 μM) and5-HT₆(EC₅₀=700 nM), an agonist at5-HT_1A(EC₅₀=3.2 μM) andD₄(EC₅₀=2 μM) receptor.

Nuciferine is a partial agonist at DD₂receptor 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_iwith a potency similar to clozapine (Nuciferine K_B=62 nM; Clozapine K_B=20 nM) as determined via Schild regression analysis^[1]. 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_Land schistosomule with 0.24±0.04 and 0.62±0.22 μM, respectively^[2].

In rodent models relevant to antipsychotic drug action, Nuciferine blocks head-twitch responses and discriminative stimulus effects of a 5-HT_2Aagonist, 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 ED₅₀value 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)^[1].

295.38

Solid

C₁₉H₂₁NO₂

475-83-2

荷叶碱

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Room temperature in continental US; may vary elsewhere.

DMSO : 5 mg/mL(16.93 mM;ultrasonic and warming and heat to 60℃)

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℃, 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。

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。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 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。