中文名称:

磷酸苯丙哌林

中文同义词:

磷酸苯丙哌啉;1-[2-(2-苄基苯氧基)-1-甲基乙基]哌啶磷酸盐;磷酸苯丙哌林;磷酸苯丙哌啉 100MG;磷酸苯丙哌林溶液,100PPM;湖北磷酸苯丙哌林原料药;磷酸苯丙哌林原料药现货;磷酸苯丙胺

英文名称:

Benproperine phosphate

英文同义词:

1-[2-(2-benzylphenoxy)-1-methylethyl]piperidine phosphate;BENPROPERINE PHOSPHATE;1-(2-Benzylphenoxy)-2-piperidinopropane phosphate;1-[2-(2-Benzylphenoxy)-1-methylethyl]piperidine monophosphate;ASA 158-5;Blascorid;Piperidine, 1-[1-methyl-2-[(a-phenyl-o-tolyl)oxy]ethyl]-, phosphate (1:1) (8CI);BENPROPERINE PHOSPHATE CP2000

CAS号:

19428-14-9

分子式:

C21H30NO5P

分子量:

407.44

EINECS号:

243-050-0

相关类别:

原料药;消化系统药物;医药与生物化工;镇咳药;化合物：原料药;医药原料 镇咳药;医药中间体;Aromatics;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals;医药原料;医药原料 镇咳药;有机原料;原料;原料;医药原料药;医药、农药及染料中间体;化学试剂

Mol文件:

19428-14-9.mol

熔点 

150-152°

CAS 数据库

19428-14-9(CAS DataBase Reference)

镇咳药

镇咳药通常分为两大类：中枢性镇咳药和外周性镇咳药。 (1) 中枢性镇咳药能够抑制延髓咳嗽中枢而产生镇咳作用，包括成瘾性镇咳药如可待因和非成瘾性镇咳药如右美沙芬、喷托维林等。 (2) 外周性镇咳药是通过抑制咳嗽反射弧中感受器、传入神经或传出神经中任何一个环节而发挥镇咳作用，如苯哌丙烷、咳快好、苯丙哌林、咳福乐、二苯哌丙烷等。 需要注意的是，镇咳药仅仅能够缓解咳嗽，但不能消除导致咳嗽的病因，只有结合病因治疗才能达到治疗的目的。无痰的干咳宜选用可待因、喷托维林或右美沙芬等药物。急性上呼吸道感染、慢性支气管炎等因素引起的咳嗽则宜选用磷酸苯丙哌林等药物。 磷酸苯丙哌林是非麻醉性镇咳药苯丙哌林的磷酸盐，外观呈白色结晶粉末，微带特臭，味苦。易溶于水、甲醇、乙酸，略溶于氯仿或苯，几乎不溶于乙醇、丙酮和乙醚。本品具有较强镇咳作用，奏效迅速，动物实验证明此药的镇咳效力比可待因强2～4倍。本品除抑制咳嗽中枢外，尚可阻断肺-胸膜的牵张感受器产生的肺-迷走神经反射，并具有罂粟碱样平滑肌解痉作用，故其镇咳作用兼具中枢性和末梢性双重机制。本品不抑制呼吸，不引起胆道及十二指肠痉挛或收缩，不引起便秘，且毒性较低，未发现耐受性及成瘾性。临床用于治疗急性支气管炎及各种原因如感染、吸烟、刺激物、过敏等引起的咳嗽，上呼吸道炎症(咽炎、鼻炎)吸烟过敏等引起的咳嗽，对刺激性干咳效佳。口服后15～60分钟内起效，持续时间为4～7小时。成人口服，每次20～40mg，1日60～120mg。也可根据病情决定。磷酸苯丙哌林副作用少，偶见口干、舌尖麻木、胃部烧灼感、食欲不振、乏力、头晕和药疹等不良反应。对本品过敏者禁用。孕妇应在医师指导下应用。

生物活性

Benproperine phosphate (Blascorid, Pirexyl) 是一种止咳药，一种口服活性的 actin-related protein 2/3 complex subunit 2 (ARPC2) 的有效抑制剂。Benproperine phosphate 会削弱 Arp2/3 功能，从而减弱肌动蛋白action的聚合成核速率。Benproperine phosphate 可抑制癌细胞迁移和肿瘤转移。

体外研究

Benproperine phosphate (20-120 μM; for 24 hours) inhibits cell viability in a dose-dependent manner. Benproperine phosphate (10 μM; for 24 hours) significantly inhibits the migration of various types of cancer cells and inhibits the migration and invasion of DLD-1, AsPC-1 cells with IC 50 values of 1-2 μM. Benproperine phosphate (10 μM; for 24 hours) does not affect cortactin-rich lamellipodium in MCF-10A cells. Cell Viability Assay Cell Line: DLD-1, AsPC-1, CFPAC-1, A375P, A375P, MDA-MB-231, DU145, DU145 cancer cells Concentration: 20, 40, 60, 80, 100, 120 μM Incubation Time: For 24 hours Result: Inhibited cell viability in a dose-dependent manner.

Cell Line:

DLD-1, AsPC-1, CFPAC-1, A375P, A375P, MDA-MB-231, DU145, DU145 cancer cells

Concentration:

20, 40, 60, 80, 100, 120 μM

Incubation Time:

For 24 hours

Result:

Inhibited cell viability in a dose-dependent manner.

体内研究

Benproperine phosphate (50, 100 mg/kg; oral gavage; 5 days per week for 4 weeks) inhibits primary pancreatic tumor growth. Benproperine phosphate shows a marked decrease in the lung metastasis of AsPC-1 cells (56.1% inhibition) in mouse. Benproperine phosphate significantly suppressed the liver metastasis of HCT-116 cells by 78.9% and DLD-1 cells by 78.2%. Animal Model: Female BALB/c nude mice of 6-week-old with AsPC-1 cells Dosage: 50, 100 mg/kg Administration: Oral gavage; 5 days per week for 4 weeks Result: Inhibited primary pancreatic tumor growth compared to the vehicle control (47.7% inhibition) without body weights change.

Animal Model:

Female BALB/c nude mice of 6-week-old with AsPC-1 cells

Dosage:

50, 100 mg/kg

Administration:

Oral gavage; 5 days per week for 4 weeks

Result:

Inhibited primary pancreatic tumor growth compared to the vehicle control (47.7% inhibition) without body weights change.

用途 

镇咳药。

用途 

用于刺激性干咳。

用途 

咳嗽药

毒性

LD50 orally in mice: 1431 mg/kg (Tellini, De Fina)