16777-42-7

• 常用中文名：盐酸奥昔非君
• 常用英文名：[R-(R*,S*)]-3-[(2-hydroxy-1-methyl-2-phenylethyl)amino]-3'-methoxypropiophenone hydrochloride
• CAS号：16777-42-7
• 分子式：C₁₉H₂₄ClNO₃
• 分子量：349.85200
• 相关类别： 原料药 循环系统用药 防治心绞痛药
• 发布时间：2018-09-20 20:48:48
• 更新时间：2024-01-02 21:43:17
• 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。

名称

• 中文名: 盐酸奥昔非君
• 英文名: 3-[[(1R,2S)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-(3-methoxyphenyl)propan-1-one,hydrochloride
• 中文别名: 安心酮盐酸盐
• 英文别名: EINECS 240-828-1; Oxyfedrine HCl; OXYFEDRINE HYDROCHLORIDE; Oxyfedrin; Oxyfedrine L-form hydrochloride; FDA 1576; l-Oxyfedrine hydrochloride; Ildamen; Modacor

物化性质

• 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

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.

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

安全

• 海关编码: 2922509090

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%