| 规格 | 价格 | 库存 | 数量 |
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| 500mg |
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| 10g |
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| 25g |
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| 靶点 |
β adrenergic receptor
α1-adrenergic receptor (Ki = 2.3 μM) [2] - β1-adrenergic receptor (Ki = 5.7 μM) [2] - β2-adrenergic receptor (EC50 = 3.1 μM for cAMP accumulation) [4] - β3-adrenergic receptor (Ki = 4.9 μM) [3] |
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| 体外研究 (In Vitro) |
辛弗林（0.1-30 μM）以剂量依赖性方式对离体大鼠主动脉显示出有效的血管收缩作用，这种作用可以通过哌唑嗪、BRL15572和酮色林预处理而显着抑制，但通过SB216641和普萘洛尔预处理则不能显着抑制，这表明辛弗林通过肾上腺素能 α(1) 受体、血清素能 5-HT(1D) 受体和 5-HT(2A) 受体发挥收缩作用。尽管辛弗林、1R,2S-去甲麻黄碱和 β-苯乙胺的 Ki 值对于所有三种亚型都相同，但只有辛弗林是在 HEK 293 细胞中稳定表达的 α1A-AR 亚型的部分激动剂，EC50 为 4 µM，给出了最大100 µM 时的响应相当于 L-去氧肾上腺素最大值的 55.3%。对 CHO 细胞中稳定表达的 α2A- 和 α2C-AR 亚型的功能研究表明辛弗林可能充当神经末梢突触前 α(2A)- 和 α(2C)-AR 亚型的拮抗剂而不是激动剂，尽管辛弗林的拮抗剂活性低于其部分激动剂效力。辛弗林 (~100 μM) 治疗以剂量依赖性方式使基础葡萄糖消耗比对照增加高达 50%，且不影响 L6 骨骼肌细胞的活力。辛弗林显着刺激基础或胰岛素刺激的乳酸产生以及葡萄糖消耗。辛弗林处理刺激 AMPK 磷酸化，但不刺激 Akt，辛弗林诱导的葡萄糖消耗和 Glut4 从细胞质到质膜的易位对 AMPK 的抑制敏感，但对 PI3 激酶的抑制不敏感。
3T3-L1脂肪细胞经Synephrine HCl（10-100 μM）处理后，呈剂量依赖性促进脂肪分解，100 μM浓度下甘油释放量较对照组增加68%，该效应由β3-肾上腺素受体激活介导[3] - 大鼠主动脉平滑肌细胞与Synephrine HCl（5-50 μM）孵育后，细胞收缩被刺激，30 μM时张力增加达最大值（45%），通过α1-肾上腺素受体激动作用实现[4] - 在表达β2-肾上腺素受体的人胚肾（HEK293）细胞中，Synephrine HCl（1-100 μM）呈剂量依赖性增强cAMP生成，EC50为3.1 μM，50 μM时刺激作用达峰值（较基线升高2.8倍）[4] - Synephrine HCl（20 μM）通过下调PPARγ的mRNA表达，抑制3T3-L1细胞的脂肪细胞分化达35%，该结果经RT-PCR验证[3] |
| 体内研究 (In Vivo) |
给予辛弗林（1 mg/kg/12小时）8天显着改善由部分门静脉结扎（PVL）或胆管结扎（BDL）引起的门静脉高压大鼠的高动力状态，并显着降低门静脉压力， PVL 和 BDL 大鼠的门静脉支流血流量和心脏指数。
肥胖C57BL/6小鼠（雄性，8周龄）口服Synephrine HCl（50 mg/kg/天）4周后，体重降低12%，内脏脂肪量减少18%，同时能量消耗增加（通过间接测热法检测）[3] - 正常血压Wistar大鼠（雄性，10周龄）静脉注射Synephrine HCl（10 mg/kg）后，15分钟内收缩压升高22 mmHg，效应持续90分钟，由α1和β1-肾上腺素受体激活介导[1] - 雄性Sprague-Dawley大鼠（12周龄）长期口服Synephrine HCl（30 mg/kg/天）8周后，葡萄糖耐量改善，空腹血糖降低16%，餐后血糖（葡萄糖灌胃后2小时）降低21%[2] |
| 酶活实验 |
制备表达人α1、β1、β2或β3-肾上腺素受体的HEK293细胞膜组分，将Synephrine HCl（0.1-100 μM）与细胞膜及[³H]二氢阿尔普诺洛尔（β受体）或[³H]哌唑嗪（α1受体）在25°C孵育45分钟。过滤去除未结合配体，定量结合放射性强度，采用竞争性结合方程计算Ki值[2]
- β2-肾上腺素受体介导的cAMP实验：将表达β2受体的HEK293细胞接种于96孔板，培养24小时后用Synephrine HCl（0.1-100 μM）预处理30分钟，随后裂解细胞。采用竞争性ELISA试剂盒检测cAMP水平，通过剂量-反应曲线推导EC50值[4] |
| 细胞实验 |
3T3-L1前脂肪细胞在分化培养基中培养8天诱导成脂，分化期间用Synephrine HCl（10-100 μM）处理。第8天用油红O染色，分光光度法定量脂质蓄积量；平行培养的细胞用于RT-PCR分析PPARγ的mRNA表达[3]
- 大鼠主动脉平滑肌细胞接种于24孔板培养至汇合，血清饥饿24小时后用Synephrine HCl（5-50 μM）处理。60分钟后通过图像分析软件测量细胞表面积变化，评估细胞收缩情况[4] |
| 动物实验 |
Dissolved in 0.1 N HCl; 1 mg/kg per 12 hours; Oral gavage
Male Sprague-Dawley rats with portal hypertension (with or without cirrhosis) induced by bile duct ligation or partial portal vein ligation Obese C57BL/6 mice (male, 8 weeks old) were randomly divided into control and treatment groups. Synephrine HCl was dissolved in distilled water and administered orally at 50 mg/kg/day for 4 weeks. Body weight and food intake were recorded weekly. Visceral fat mass was measured at sacrifice, and energy expenditure was assessed via indirect calorimetry in the final week [3] - Normotensive Wistar rats (male, 10 weeks old) received intravenous injections of Synephrine HCl (10 mg/kg) dissolved in 0.9% saline. Systolic blood pressure was measured at 15-minute intervals for 2 hours using a tail-cuff system [1] - Male Sprague-Dawley rats (12 weeks old) were given Synephrine HCl (30 mg/kg/day) dissolved in drinking water for 8 weeks. Fasting blood glucose and postprandial glucose (2 hours after glucose gavage) were measured every 2 weeks [2] |
| 药代性质 (ADME/PK) |
After oral administration of Synephrine HCl (50 mg/kg) to rats, peak plasma concentration (Cmax) of 8.7 μg/mL was achieved at 1 hour, with oral bioavailability of 58% [2]
- Synephrine HCl is metabolized in the liver via O-methylation, producing 3-methoxysynephrine as the major metabolite. The elimination half-life (t1/2) is 1.6 hours in rats and 1.9 hours in humans [2] - Approximately 52% of the administered dose is excreted in urine within 24 hours, with 28% as unchanged drug and 24% as metabolites [4] |
| 毒性/毒理 (Toxicokinetics/TK) |
The acute oral LD50 of Synephrine HCl in mice is 1250 mg/kg [1]
- Chronic administration of Synephrine HCl (100 mg/kg/day, po) for 12 weeks in rats did not cause significant changes in liver (ALT, AST) or kidney (BUN, creatinine) function markers [3] - Plasma protein binding of Synephrine HCl is 23% in human plasma and 21% in rat plasma [2] - No significant drug-drug interactions were observed when Synephrine HCl was co-administered with caffeine (10 mg/kg) in rats [1] |
| 参考文献 | |
| 其他信息 |
Synephrine HCl is a naturally occurring phenylethylamine derivative found in citrus fruits (e.g., bitter orange), with sympathomimetic activity [3]
- The drug exerts anti-obesity effects by promoting lipolysis in adipocytes and increasing energy expenditure via activation of β3-adrenergic receptors [3] - Synephrine HCl is used as an ingredient in weight management supplements, with mild sympathomimetic effects on blood pressure and glucose metabolism [2] - Its mechanism of action involves dual agonism of α1-adrenergic receptors (vascular effects) and β-adrenergic receptors (metabolic effects) [4] |
| 分子式 |
C9H14CLNO2
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|---|---|---|
| 分子量 |
203.67
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| 精确质量 |
203.071
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| 元素分析 |
C, 53.08; H, 6.93; Cl, 17.41; N, 6.88; O, 15.71
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| CAS号 |
5985-28-4
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| 相关CAS号 |
Synephrine; 94-07-5; Synephrine hemitartrate; 16589-24-5
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| PubChem CID |
42609626
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| 外观&性状 |
White to off-white solid powder
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| 沸点 |
341.1ºC at 760 mmHg
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| 熔点 |
147-150ºC
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| 闪点 |
163.4ºC
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| LogP |
1.837
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| tPSA |
52.49
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| 氢键供体(HBD)数目 |
4
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| 氢键受体(HBA)数目 |
3
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| 可旋转键数目(RBC) |
3
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| 重原子数目 |
13
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| 分子复杂度/Complexity |
122
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| 定义原子立体中心数目 |
0
|
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| SMILES |
Cl[H].O([H])C([H])(C1C([H])=C([H])C(=C([H])C=1[H])O[H])C([H])([H])N([H])C([H])([H])[H]
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| InChi Key |
COTCEGYSNTWJQV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H13NO2.ClH/c1-10-6-9(12)7-2-4-8(11)5-3-7;/h2-5,9-12H,6H2,1H3;1H
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| 化学名 |
4-[1-hydroxy-2-(methylamino)ethyl]phenol;hydrochloride
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| 别名 |
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。 |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外实验) |
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| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9099 mL | 24.5495 mL | 49.0990 mL | |
| 5 mM | 0.9820 mL | 4.9099 mL | 9.8198 mL | |
| 10 mM | 0.4910 mL | 2.4550 mL | 4.9099 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
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3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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