荷叶碱 T3369

Product Introduction
Bioactivity


英文名: Nuciferine

描述: Nuciferine ((-)-Nuciferine) 是一种在埃及蓝睡莲和水芙蓉中发现的生物碱，是5-HT2A、5-HT2B 和5-HT2C 拮抗剂，IC50分别为 478 nM、1 μM 和 131 nM。它也是5-HT7的反向激动剂，IC50为 150 nM。

细胞实验: Nuciferine is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. Cells are plated into 48-well plates one day before uptake is performed. Cells are washed with 0.5 mL uptake buffer (4 mM Tris, 6.25 mM HEPES, 120 mM NaCl, 5 mM KCl, 1.2 mM CaCl2, 1.2 mM MgSO4, 5.6 mM D-glucose, 1.7 mM ascorbic acid, and 1 μM pargyline, pH 7.4). Cells are incubated with 225 μL uptake buffer with or without the indicated concentration of Nuciferine for 15 minutes. After incubation, 25 μL uptake buffer containing 3H-DA and DA is added for a final concentration of 20 nM 3H-DA and 1 μM DA. Cells are incubated at 37°C for 20 minutes or for the time indicated. Nonspecific uptake is determined in the presence of 10 μM nomifensine. Uptake is terminated by aspirating uptake buffer and washing each well twice with 0.5 mL ice-cold uptake buffer. Cells are lysed in 0.1 N NaOH and transferred to vials containing 3 mL scintillation cocktail. Radioactivity is quantitated using a Beckman LS6500 counter. Data are analyzed in Graph Pad Prism 5.0[1].

激酶实验: For affinity determination, Nuciferine is subjected to primary radioligand binding assays tested at a single 10 μM concentration to displace 50% of the radioligand at a given receptor target. If a more than 50% of the radioligand is displaced, Nuciferine is selected for a secondary binding assay tested at 11 concentrations in triplicate in competition with the radioligand to generate an IC50 and Ki. Binding assays are performed in 96-well plates with 125 μL per well in appropriate binding buffer using radioligand at or near the Kd. Plates are incubated at room temperature in the dark for 90 min. Reactions are stopped by vacuum filtrations onto 0.3% polyethyleneimine soaked 96-well filter mats using a 96-well Filtermate harvester, followed by at least three washes of cold wash buffer. Scintillation cocktail is melted onto dried filters and radioactivity is counted using a Wallac Trilux Microbeta[1].

体外活性: Nuciferine is a partial agonist at DD2 receptor with an activity (Emax=67% of dopamine) similar to aripiprazole (Emax=50% of dopamine). In line with its partial agonist activity, Nuciferine inhibited dopamine-induced activation of Gi with a potency similar to clozapine (Nuciferine KB=62 nM; Clozapine KB=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.5HTRL and schistosomule with 0.24±0.04 and 0.62±0.22 μM, respectively[2].

体内活性: In rodent models relevant to antipsychotic drug action, Nuciferine blocks head-twitch responses and discriminative stimulus effects of a 5-HT2A 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 clozapines 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 2.95 mg/mL (10 mM)


关键字: Inhibitor | 5-hydroxytryptamine Receptor | Dopamine Receptor | 5-HT Receptor | Serotonin Receptor | VLT-049 | Nuciferine | inhibit | VLT049

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相关库: Anti-Neurodegenerative Disease Compound Library | Anti-Parkinson's Disease Compound Library | Anti-Cancer Compound Library | FDA-Approved & Pharmacopeia Drug Library | Membrane Protein-targeted Compound Library | Antidepressant Compound Library | Inhibitor Library | GPCR Compound Library | Serotonin Receptor-Targeted Compound Library | Traditional Chinese Medicine Monomer Library

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