525-66-6

• 常用中文名：心得安(普萘洛尔)
• 常用英文名：propranolol
• CAS号：525-66-6
• 分子式：C₁₆H₂₁NO₂
• 分子量：259.34300
• 相关类别： 原料药 循环系统用药 抗心律失常药
• 发布时间：2018-02-04 08:00:00
• 更新时间：2024-01-02 19:53:39
• Propranolol 普萘洛尔是一种非心脏选择性 β 受体阻滞剂 β-blocker。Propranolol 具有膜稳定性质,但不具有内在的拟交感神经活性。Propranolol 用于控制高血压,嗜铬细胞瘤,心肌梗塞,心律失常,心绞痛和肥厚性心肌病。
• 普萘洛尔(心得安)与去甲肾上腺素能神经递质或拟肾上腺素因药物竞争β受体，从而抑制去甲肾上腺素能经神支配器官的β效应。
  ⒈心血管 对心脏β1受体阻断作用较强，可使心率减慢，心肌收缩力减弱；能降低心肌自律性，延长有效不应期（effective refractory period,ERP），减慢传导，使心输出量减少，心肌耗氧降低，血压稍降低。心得安对心脏抑制作用强度与心脏交感神经的张力大小有关，如运动、病理状态时交感神经的张力增高，心得安对心脏的抑制作用较强，对正常人休息时心脏作用较弱。心得安可反射性引起外周阻力增加，使内脏（肝、肾等）器官血流减少，冠脉流量亦降低。
  ⒉支气管平滑肌阻断β2受体，可使支气管平滑肌收缩，对支气管哮喘患者可诱发或加重急性发作。
  ⒊其他 ①内在拟交感神经活动性，有些β受体阻断药物尚有一定程度的兴奋β受体的性能，这种性能是内在拟交感活动性所引起的β受体兴奋效应，往往被β受体阻断效应所掩盖，但可以对抗或减弱β型应用的效果；②膜定作用，有些β受体阻断剂尚有局部麻醉和直接抑制心脏作用（奎尼丁样作用）。这两种作用都是由于稳定细胞膜，使神经纤维或心肌细胞膜对阳离子的通透性降低所致，故统称为膜定作用。

名称

• 中文名: 心得安(普萘洛尔)
• 英文名: propranolol
• 中文别名: 1-异丙基氨基-3-(萘-1-氧基)丙-2-醇; 心得安; 萘心安; 恩得来; 萘氧丙醇胺; 普萘洛尔
• 英文别名: Disoprivan; Propranolol; Fresofol; 2,6-diisopropylphenol; 2-Propanol,1-[(1-methylethyl)amino]-3-(1-naphthalenyloxy)-; Propofolum; Disoprofol; Diprivan; 2-hydroxy-1,3-diisopropylbenzene; propofol; 2,6-i-Pr2-C6H3-OH; Diisopropylphenol

物化性质

• 密度: 1.093 g/cm3
• 沸点: 434.9ºC at 760 mmHg
• 熔点: 163-164ºC
• 分子式: C₁₆H₂₁NO₂
• 分子量: 259.34300
• 闪点: 216.8ºC
• 精确质量: 259.15700
• PSA: 41.49000
• LogP: 2.96840
• 外观性状: 白色,无气味的结晶粉末
• 折射率: 1.5500 (estimate)
• 储存条件: 室温

生物活性

• 描述: Propranolol 普萘洛尔是一种非心脏选择性 β 受体阻滞剂 β-blocker。Propranolol 具有膜稳定性质,但不具有内在的拟交感神经活性。Propranolol 用于控制高血压,嗜铬细胞瘤,心肌梗塞,心律失常,心绞痛和肥厚性心肌病。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 其他 >> 其他
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Al-Majed AA, et al. Propranolol. Profiles Drug Subst Excip Relat Methodol. 2017;42:287-338.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UB7500000 CHEMICAL NAME : 2-Propanol, 1-(isopropylamino)-3-(1-naphthyloxy)- CAS REGISTRY NUMBER : 525-66-6 LAST UPDATED : 199709 DATA ITEMS CITED : 29 MOLECULAR FORMULA : C16-H21-N-O2 MOLECULAR WEIGHT : 259.38 WISWESSER LINE NOTATION : L66J BO1YQ1MY1&1 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 708 mg/kg/39W-I TOXIC EFFECTS : Nutritional and Gross Metabolic - other changes TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 3200 ug/kg/2D-I TOXIC EFFECTS : Endocrine - hypoglycemia TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human DOSE/DURATION : 2300 ug/kg/D TOXIC EFFECTS : Behavioral - hallucinations, distorted perceptions TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 120 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - child DOSE/DURATION : 800 ug/kg/12H TOXIC EFFECTS : Cardiac - pulse rate increase, without fall in BP Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - acute pulmonary edema TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - child DOSE/DURATION : 400 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Cardiac - arrhythmias (including changes in conduction) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 8343 mg/kg/4Y-I TOXIC EFFECTS : Endocrine - evidence of thyroid hyperfunction TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human DOSE/DURATION : 71 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Unreported SPECIES OBSERVED : Human - man DOSE/DURATION : 22857 ug/kg/40D-I TOXIC EFFECTS : Sense Organs and Special Senses (Ear) - change in acuity TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 660 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 23 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 289 mg/kg TOXIC EFFECTS : Autonomic Nervous System - beta-adrenergic blockage TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 42 mg/kg TOXIC EFFECTS : Autonomic Nervous System - beta-adrenergic blockage TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 150 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 28100 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 120 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 40 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 26 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 7 gm/kg/35D-C TOXIC EFFECTS : Liver - other changes Kidney, Ureter, Bladder - other changes Blood - changes in spleen TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1096 mg/kg SEX/DURATION : female 1-40 week(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Specific Developmental Abnormalities - blood and lymphatic systems (including spleen and marrow) Reproductive - Effects on Newborn - Apgar score (human only) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Multiple routes DOSE : 932 mg/kg SEX/DURATION : female 4-40 week(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - Apgar score (human only) Reproductive - Effects on Newborn - other neonatal measures or effects Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 966 mg/kg SEX/DURATION : male 6 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 650 mg/kg SEX/DURATION : female 8-20 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 325 mg/kg SEX/DURATION : female 8-20 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - biochemical and metabolic TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous DOSE : 1 mg/kg SEX/DURATION : female 8 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - uterus, cervix, vagina TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Unreported DOSE : 300 mg/kg SEX/DURATION : female 10-12 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetal death MUTATION DATA TEST SYSTEM : Rodent - mouse DOSE/DURATION : 74500 ug/kg REFERENCE : MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 173,207,1986 *** REVIEWS *** TOXICOLOGY REVIEW FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 6,395,1986 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4181 No. of Facilities: 17 (estimated) No. of Industries: 2 No. of Occupations: 7 No. of Employees: 1785 (estimated) No. of Female Employees: 355 (estimated)

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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%