化学信息:
中文名 | 荷叶碱 |
英文名 | Nuciferine |
中文别名 | - |
英文别名 | Sanjoinine E |
来源 | 莲Nelumbo nucifera Gaertn. |
化合物类型 | 生物碱(Alkaloids)>异喹啉类生物碱 |
化学式 | C19H21NO2 |
分子量 | 295.38 |
CAS号 | 475-83-2 |
纯度 | 98%, HPLC |
溶剂/溶解度 |
Water: < 0.1 mg/ml (insoluble); 0.1>DMSO: 11.11 mg/ml (37.61 mM) |
溶液配制 | 5mg加入1.69ml DMSO,或者每2.95mg加入1ml DMSO,配制成10mM溶液。 |
生物信息
产品描述 | Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (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-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor. | ||||
信号通路 | - | ||||
靶点 | 5-HT2B Receptor | D4 Receptor | D5 Receptor | 5-HT1A Receptor | D2 Receptor |
IC50 | 1 μM | 2 μM | 2.6 μM | 3.2 μM | 64 μM |
体外研究 | 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. 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. | ||||
体内研究 | 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 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). | ||||
临床实验 | N/A |
1. Farrell MS, et al. PLoS One. 2016,11(3):e0150602.
2. Chan JD, et al. Int J Parasitol Drugs Drug Resist. 2016,6(3):364-370.
包装清单:产品编号 | 产品名称 | 包装 |
SM4084-10mM | 荷叶碱(98%, HPLC) | 10mM×0.2ml |
SM4084-5mg | 荷叶碱(98%, HPLC) | 5mg |
SM4084-25mg | 荷叶碱(98%, HPLC) | 25mg |
SM4084-100mg | 荷叶碱(98%, HPLC) | 100mg |
- | 说明书 | 1份 |
-20℃保存,至少一年有效。固体粉末4℃保存,至少一个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:本产品可能对人体有一定的毒害作用,请注意适当防护,以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
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