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药品详细

Bopindolol(波吲洛尔)

化学结构式图
中文名
波吲洛尔
英文名
Bopindolol
分子式
C23H28N2O3
化学名
1-(tert-butylamino)-3-[(2-methyl-1H-indol-4-yl)oxy]propan-2-yl benzoate
分子量
Average: 380.48
Monoisotopic: 380.209992772
CAS号
69010-88-4
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

Bopindolol (INN) is a beta blocker. It is an ester which acts as a prodrug for pindolol.

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    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 Not Available
    Substructures Not Available
    适应症
    药理
    Indication For the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation.
    Pharmacodynamics Bopindolol is a prodrug of pindolol. Pindolol is a non-selective beta-adrenergic antagonist (beta-blocker) which possesses intrinsic sympathomimetic activity (ISA) in therapeutic dosage ranges but does not possess quinidine-like membrane stabilizing activity. Pindolol impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Pindolol is nonpolar and hydrophobic, with low to moderate lipid solubility. Pindolol has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, pindolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action.
    Mechanism of action Bopindolol (as pindolol) 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. By binding beta-2 receptors in the juxtaglomerular apparatus, Pindolol 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 Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 152–153 [malonate salt] MSDS
    water solubility 3.3 mg/ml (malonate salt) Not Available
    Predicted Properties
    Property Value Source
    water solubility 1.60e-03 g/l ALOGPS
    logP 4.45 ALOGPS
    logP 4.67 ChemAxon
    logS -5.4 ALOGPS
    pKa (strongest acidic) 16.8 ChemAxon
    pKa (strongest basic) 9.29 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 63.35 ChemAxon
    rotatable bond count 9 ChemAxon
    refractivity 111.07 ChemAxon
    polarizability 43.08 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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