19428-14-9
19428-14-9 結(jié)構(gòu)式
基本信息
磷酸苯丙哌林
磷酸苯丙哌啉
BENPROPERINE PHOSPHATE
BENPROPERINE PHOSPHATE CP2000
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)
Piperidine, 1-[1-methyl-2-[2-(phenylmethyl)phenoxy]ethyl]-, phosphate (1:1)
Flaveric
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見問題列表
(1) 中樞性鎮(zhèn)咳藥能夠抑制延髓咳嗽中樞而產(chǎn)生鎮(zhèn)咳作用，包括成癮性鎮(zhèn)咳藥如可待因和非成癮性鎮(zhèn)咳藥如右美沙芬、噴托維林等。
(2) 外周性鎮(zhèn)咳藥是通過抑制咳嗽反射弧中感受器、傳入神經(jīng)或傳出神經(jīng)中任何一個(gè)環(huán)節(jié)而發(fā)揮鎮(zhèn)咳作用，如苯哌丙烷、咳快好、苯丙哌林、咳福樂、二苯哌丙烷等。
需要注意的是，鎮(zhèn)咳藥僅僅能夠緩解咳嗽，但不能消除導(dǎo)致咳嗽的病因，只有結(jié)合病因治療才能達(dá)到治療的目的。無痰的干咳宜選用可待因、噴托維林或右美沙芬等藥物。急性上呼吸道感染、慢性支氣管炎等因素引起的咳嗽則宜選用磷酸苯丙哌林等藥物。
磷酸苯丙哌林是非麻醉性鎮(zhèn)咳藥苯丙哌林的磷酸鹽，外觀呈白色結(jié)晶粉末，微帶特臭，味苦。易溶于水、甲醇、乙酸，略溶于氯仿或苯，幾乎不溶于乙醇、丙酮和乙醚。本品具有較強(qiáng)鎮(zhèn)咳作用，奏效迅速，動(dòng)物實(shí)驗(yàn)證明此藥的鎮(zhèn)咳效力比可待因強(qiáng)2～4倍。本品除抑制咳嗽中樞外，尚可阻斷肺-胸膜的牽張感受器產(chǎn)生的肺-迷走神經(jīng)反射，并具有罌粟堿樣平滑肌解痙作用，故其鎮(zhèn)咳作用兼具中樞性和末梢性雙重機(jī)制。本品不抑制呼吸，不引起膽道及十二指腸痙攣或收縮，不引起便秘，且毒性較低，未發(fā)現(xiàn)耐受性及成癮性。臨床用于治療急性支氣管炎及各種原因如感染、吸煙、刺激物、過敏等引起的咳嗽，上呼吸道炎癥(咽炎、鼻炎)吸煙過敏等引起的咳嗽，對(duì)刺激性干咳效佳?？诜?5～60分鐘內(nèi)起效，持續(xù)時(shí)間為4～7小時(shí)。成人口服，每次20～40mg，1日60～120mg。也可根據(jù)病情決定。磷酸苯丙哌林副作用少，偶見口干、舌尖麻木、胃部燒灼感、食欲不振、乏力、頭暈和藥疹等不良反應(yīng)。對(duì)本品過敏者禁用。孕婦應(yīng)在醫(yī)師指導(dǎo)下應(yīng)用。
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. |
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. |