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药品详细

Bupranolol(布拉洛尔)

化学结构式图
中文名
布拉洛尔
英文名
Bupranolol
分子式
C14H22ClNO2
化学名
tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine
分子量
Average: 271.783
Monoisotopic: 271.13390666
CAS号
23284-25-5
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

Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar to propranolol.

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 Not Available
    Substructures Not Available
    适应症
    药理
    Indication Used to manage hypertension and tachycardia. Also used to treat glaucoma.
    Pharmacodynamics Bupranolol is a competitive, nonselective beta-blocker similar to propanolol without intrinsic sympathomimetic activity.
    Mechanism of action Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.
    Absorption Quickly and completely absorbed from the gut with less than 10% oral bioavailability.
    Volume of distribution Not Available
    Protein binding 76%
    Metabolism
    Over 90% undergo first-pass metabolism. The main metabolite is carboxybupranolol, 4-chloro-3-[3-(1,1-dimethylethylamino)-2-hydroxy-propyloxy]benzoic acid, of which 88% are eliminated renally within 24 hours.

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

    Substrate Enzymes Product
    Bupranolol
      		carboxybupranolol, 4-chloro-3-[3-(1,1-dimethylethylamino)-2-hydroxy-propyloxy]benzoic acid Details
      Route of elimination Not Available
      Half life 2-4 hours
      Clearance Not Available
      Toxicity Symptoms of overdose include bradycardia, cardiac failure, hypotension, and brochospasm.
      Affected organisms
      • Humans and other mammals
      Pathways Not Available
      理化性质
      Properties
      State solid
      Experimental Properties Not Available
      Predicted Properties
      Property Value Source
      water solubility 1.43e-01 g/l ALOGPS
      logP 3.14 ALOGPS
      logP 2.99 ChemAxon
      logS -3.3 ALOGPS
      pKa (strongest acidic) 14.09 ChemAxon
      pKa (strongest basic) 9.76 ChemAxon
      physiological charge 1 ChemAxon
      hydrogen acceptor count 3 ChemAxon
      hydrogen donor count 2 ChemAxon
      polar surface area 41.49 ChemAxon
      rotatable bond count 6 ChemAxon
      refractivity 74.86 ChemAxon
      polarizability 30.35 ChemAxon
      药物相互作用
      食物相互作用
      Not Available

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