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药品详细

Alprenolol(心安)

化学结构式图
中文名
心安
英文名
Alprenolol
分子式
C15H23NO2
化学名
{2-hydroxy-3-[2-(prop-2-en-1-yl)phenoxy]propyl}(propan-2-yl)amine
分子量
Average: 249.3486
Monoisotopic: 249.172878985
CAS号
13655-52-2
ATC分类
C07A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

One of the adrenergic beta-antagonists used as an antihypertensive, anti-anginal, and anti-arrhythmic agent. [PubChem]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Phenols and Derivatives
    • Ethers
    • Anisoles
    • Phenyl Esters
    Substructures
    • Hydroxy Compounds
    • Alkanes and Alkenes
    • Aliphatic and Aryl Amines
    • Phenols and Derivatives
    • Ethers
    • Benzene and Derivatives
    • Amino Alcohols
    • Aromatic compounds
    • Anisoles
    • Alcohols and Polyols
    • Phenyl Esters
    适应症
    药理
    Indication For the treatment of hypertension, angina, and arrhythmia
    Pharmacodynamics Alprenolol is a non-selective beta-blocker used in the treatment of hypertension, edema, ventricular tachycardias, and atrial fibrillation. Alprenolol impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Alprenolol is nonpolar and hydrophobic, with low to moderate lipid solubility. Alprenolol has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, alprenolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action.
    Mechanism of action Alprenolol non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. Also, with a more minor effect, by binding beta-2 receptors in the juxtaglomerular apparatus, alprenolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding 80-90%
    Metabolism
    Hepatic. One of the active metabolites, 4-OH-alprenolol, is an active beta-blocker.

    Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

    Substrate Enzymes Product
    Alprenolol
      		4-hydroxy-alprenolol Details
      Route of elimination Not Available
      Half life 2-3 hours
      Clearance Not Available
      Toxicity LD50=597.0 mg/kg (Orally in rats)
      Affected organisms
      • Humans and other mammals
      Pathways
      Pathway Name SMPDB ID
      Smp00297 Alprenolol Pathway SMP00297
      理化性质
      Properties
      State solid
      Experimental Properties
      Property Value Source
      melting point 107-109 °C PhysProp
      water solubility 547 mg/L Not Available
      logP 3.10 HANSCH,C ET AL. (1995)
      Caco2 permeability -4.62 ADME Research, USCD
      Predicted Properties
      Property Value Source
      water solubility 1.88e-01 g/l ALOGPS
      logP 2.59 ALOGPS
      logP 2.69 ChemAxon
      logS -3.1 ALOGPS
      pKa (strongest acidic) 14.09 ChemAxon
      pKa (strongest basic) 9.67 ChemAxon
      physiological charge 1 ChemAxon
      hydrogen acceptor count 3 ChemAxon
      hydrogen donor count 2 ChemAxon
      polar surface area 41.49 ChemAxon
      rotatable bond count 8 ChemAxon
      refractivity 74.66 ChemAxon
      polarizability 29.38 ChemAxon
      药物相互作用
      食物相互作用
      Not Available

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