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盐酸奥昔非君

盐酸奥昔非君用途

Oxyfedrine hydrochloride,一种血管扩张剂,是一种具有口服活性的 β-肾上腺素受体 (β-adrenoreceptor) 激动剂。Oxyfedrine hydrochloride 可降低冠状血管的张力。Oxyfedrine 可用于心血管疾病的研究。

盐酸奥昔非君名称

[ CAS 号 ]:
16777-42-7

[ 中文名 ]:
盐酸奥昔非君

[ 英文名 ]:
[R-(R*,S*)]-3-[(2-hydroxy-1-methyl-2-phenylethyl)amino]-3'-methoxypropiophenone hydrochloride

[中文别名 ]:

[英文别名 ]:

盐酸奥昔非君生物活性

[ 描述 ]:

Oxyfedrine hydrochloride,一种血管扩张剂,是一种具有口服活性的 β-肾上腺素受体 (β-adrenoreceptor) 激动剂。Oxyfedrine hydrochloride 可降低冠状血管的张力。Oxyfedrine 可用于心血管疾病的研究。

[ 相关类别 ]:

研究领域 >> 心血管疾病
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

[体外研究]

羟苯丙胺(50μM,48小时)抑制HCT116和HSC-4细胞中的乙醛脱氢酶(ALDH)活性[1]。Oxyfederine(50μM,48小时)作为GSH消耗剂的敏化剂,与药物组合使用时可诱导HCT116和HSC-4细胞死亡[1]。Oxyfederine(0-1μg/mL)抑制大鼠离体门静脉的自发肌源性活动[4]。

[体内研究]

Oxyfederine(14 mg/kg,口服,持续3-4周)在猫中显示出抗心绞痛作用[2]。当与柳氮磺胺吡啶(SSZ,350 mg/kg,i.p.)联合使用时,奥替尼(10 mg/kg,i.p.HCT116细胞异种移植物小鼠)抑制肿瘤生长[1]。奥替尼可降低冰水应激大鼠的动脉和静脉血液高血粘度(HBV)[3]。

[参考文献]

[1]. Otsuki Y, et al. Vasodilator oxyfedrine inhibits aldehyde metabolism and thereby sensitizes cancer cells to xCT-targeted therapy. Cancer Sci. 2020 Jan;111(1):127-136.  

[2]. Parratt JR. The haemodynamic effects of prolonged oral administration of oxyfedrine, a partial agonist at beta-adrenoceptors: comparison with propranolol. Br J Pharmacol. 1974 May;51(1):5-13.  

[3]. Yu J, et al. [Effects of oxyfedrine on high blood viscosity and myocardial necrosis induced by epinephrine and ice water stress in rats]. Zhongguo Yao Li Xue Bao. 1993 Jul;14(4):364-6.  

[4]. Mackenzie JE, et al. Effects of oxyfedrine on isolated portal vein and other smooth muscles. Br J Pharmacol. 1973 Apr;47(4):827-37.  

盐酸奥昔非君物理化学性质

[ 密度 ]:
1.122g/cm3

[ 沸点 ]:
475.2ºC at 760mmHg

[ 熔点 ]:
192-194℃

[ 分子式 ]:
C19H24ClNO3

[ 分子量 ]:
349.85200

[ 精确质量 ]:
349.14400

[ PSA ]:
58.56000

[ LogP ]:
4.17260

[ 蒸汽压 ]:
7.78E-10mmHg at 25°C

盐酸奥昔非君毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UH2450000
CHEMICAL NAME :
Propiophenone, 3-((beta-hydroxy-alpha-methylphenethyl)amino)-3'-meth oxy-, hydrochloride, (-)-
CAS REGISTRY NUMBER :
16777-42-7
LAST UPDATED :
199109
DATA ITEMS CITED :
13
MOLECULAR FORMULA :
C19-H23-N-O3.Cl-H
MOLECULAR WEIGHT :
349.89
WISWESSER LINE NOTATION :
QYR&Y1&M2VR CO1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,1478,1967
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
92 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,1478,1967
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
99 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,152,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
46 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,1478,1967
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
510 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,1478,1967
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
95 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,1478,1967
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
123 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,152,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
23 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 27,1401,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
200 mg/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - ataxia Cardiac - pulse rate
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,1478,1967
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
50 mg/kg
TOXIC EFFECTS :
Behavioral - muscle contraction or spasticity
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,1478,1967
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
21200 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,1478,1967
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
340 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,1478,1967
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
83 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 17,1478,1967

盐酸奥昔非君安全信息

[ 海关编码 ]:
2922509090

盐酸奥昔非君海关

[ 海关编码 ]: 2922509090

[ 中文概述 ]:
2922509090. 其他氨基醇酚、氨基酸酚及其他含氧基氨基化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件：AB. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: R.进口食品卫生监督检验 S.出口食品卫生监督检验

[ Summary ]:
2922509090. other amino-alcohol-phenols, amino-acid-phenols and other amino-compounds with oxygen function. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

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