中文名称:

四氢帕马丁

中文同义词:

四氢帕马丁;左旋四氢巴马亭;L-四氢巴马亭;消旋延胡索乙素;延胡索乙素, 来源于延胡索;罗通宝;罗通定(四氢帕马丁);消旋延胡索乙素(标准品)

英文名称:

Tetrahydropalmatine

英文同义词:

TETRAHYDROPALMATINE, L-;(S)-2,3,9,10-TETRAMETHOXY-5,8,13,13A-TETRAHYDRO-6H-ISOQUINO[3,2-A]ISOQUINOLINE;2,3,9,10-tetramethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinoline;ROTUNDINUM;ROTUNDIN HYDRATE;AKOS 208-04;L-TETRAHYDROPALMATINE;TETRAHYDROPALMITINE

CAS号:

2934-97-6

分子式:

C21H25NO4

分子量:

355.43

EINECS号:

相关类别:

植物生化提取物;中药标准品;小分子抑制剂，天然产物;小分子抑制剂;植物提取物;对照品,标准品;分析标准品;中草药成分;标准品;对照品;中药对照品;植提标准品;Inhibitors;分析试剂-对照品

Mol文件:

2934-97-6.mol

熔点 

155℃

沸点 

482.9±45.0 °C(Predicted)

密度 

1.23±0.1 g/cm3(Predicted)

储存条件 

Sealed in dry,Room Temperature

酸度系数(pKa)

6.53±0.20(Predicted)

简介

四氢帕马丁即四氢巴马汀，可由四羟基黄连总碱制备得到。四氢帕马丁可用于制备巴马汀。巴马汀具有广谱抗菌作用，尤其是对于抗白色念珠菌，临床上可用于治疗妇科炎症、菌痢、肠炎、呼吸道和泌尿道感染、外科感染及结膜炎等。

用途

四氢帕马丁具有镇痛、镇静、催眠及安定作用，镇痛作用不及呱替啶，但比一般解热镇痛药强。dl -四氢帕马丁是中药延胡索的主要活性物质，通过拮抗纹状体多巴胺D2受体能引起大鼠低血压和心动过缓。

制备

A、盐酸小檗碱在对甲苯磺酸、二甲苯、HCl，70℃条件下开环得到去亚甲基盐酸小檗碱。 B、去亚甲基盐酸小檗碱在碳酸钾、甲醇、硫酸二甲酯，40℃条件下甲醚化得到盐酸巴马汀。 C、盐酸巴马汀在甲醇、硼氢化钠条件下消旋得到四氢帕马丁。

生物活性

Tetrahydropalmatine 是从延胡索中提取的有效成分，具有镇痛作用。Tetrahydropalmatine 通过抑制大鼠杏仁核的多巴胺释放来抑制癫痫发作。

靶点

Dopamine

体内研究

Tetrahydropalmatine (THP), an active component isolated from corydalis (a Chinese herbal medicine), possesses analgesic effects. Picrotoxin treatment alone has a significant effect on the following activity measure: there is an increase in horizontal motion time (HMT), vertical motion time (VMT), clockwise turnings (CT), anticlockwise turning (ACT) and a decrease in freezing time (FT). Tetrahydropalmatine treatment alone causes a decrease in HMT, VMT and total distance traveled (TDT), but an increase in FT. Pretreatment of rats with an i.p. dose of 10 mg/kg or 15 mg/kg of Tetrahydropalmatine significantly attenuates the Picrotoxin-induced enhancement in HMT, VMT, CT, ACT and TDT, as well as reduction in FT. Another 48 rats under urethane anesthesia are randomly divided into six groups, each of eight rats. The s.c. injection of Picrotoxin causes an increase in amygdaloid release of dopamine (DA), while i.p. injection of Tetrahydropalmatine at 10 mg/kg has an insignificant effect on amygdaloid release of DA. Again, the Picrotoxin-induced increase in amygdaloid release of DA is significantly attenuated by pretreatment with Tetrahydropalmatine. The Picrotoxin-induced augmented amygdaloid release of DA is almost completely abolished by pretreatment with Tetrahydropalmatine 30 min before s.c. injection of Picrotoxin.

用途 

用作镇痛药，适用于内科疾病引起的胃肠道和肝胆系统的头痛、痛经及分娩止痛

海关编码 

29339900