荷叶碱
荷叶碱 性质
熔点 | 165.5°C |
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沸点 | 437.06°C (rough estimate) |
密度 | 1.1156 (rough estimate) |
折射率 | 1.5000 (estimate) |
储存条件 | 2-8°C |
溶解度 | DMSO : 11.11 mg/mL (37.61 mM; 需要超声波)H2O : < 0.1 mg/mL (不溶) |
酸度系数(pKa) | 7.87±0.20(Predicted) |
形态 | 粉末 |
颜色 | 白色至米色 |
旋光性 (optical activity) | [α]/D -145 to -165°, c = 0.5 in ethanol |
LogP | 2.357 (est) |
荷叶碱 用途与合成方法
中医学认为,荷叶性味苦涩,平,归肝、脾、胃、心经。有清暑利湿、升发清阳、凉血止血等功效。荷叶的主要化学成分有荷叶碱、柠檬酸、草酸等,起主要减肥作用的是荷叶碱,药理研究表明,荷叶具有利尿通便、通肠毒、降脂除油、清暑解热等作用,能明显降低血清中甘油三醇和胆固醇含量,具有调节血脂的保健作用。采用荷叶减肥不需要刻意节食,对人体无任何副作用。 Nuciferine 是一种 5-HT2A,5-HT2C 和 5-HT2B 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。
5-HT 2C Receptor 131 nM (IC 50 ) |
5-HT 7 Receptor 150 nM (IC 50 ) |
5-HT 2A Receptor 478 nM (IC 50 ) |
5-HT 2B Receptor 1 μM (IC 50 ) |
5-HT 6 Receptor 700 nM (EC 50 ) |
5-HT 1A Receptor 3.2 μM (EC 50 ) |
D 2 Receptor 64 nM (EC 50 ) |
D 4 Receptor 2 μM (EC 50 ) |
D 5 Receptor 2.6 μM (EC 50 ) |
Nuciferine is a partial agonist at DD 2 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.
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 ED 50 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).
药理药效:具有减肥降脂的作用。
安全信息
安全说明 | 24/25 |
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危险品运输编号 | UN 1544PSN1 6.1 / PGIII |
海关编码 | 29389090 |
毒性 | LD50 orl-rat: 280 mg/kg AIPTAK 197,261,72 |
荷叶碱 化学药品说明书
荷叶碱 价格(试剂级)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024-11-08 | HY-N0049 | 荷叶碱 | 475-83-2 | 5mg | 500 |
2024-11-08 | HY-N0049 | 荷叶碱 | 475-83-2 | 10mM * 1mLin DMSO | 550 |