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药品详细

Arbutamine(阿布他明)

化学结构式图
中文名
阿布他明
英文名
Arbutamine
分子式
C18H23NO4
化学名
4-[(1R)-1-hydroxy-2-{[4-(4-hydroxyphenyl)butyl]amino}ethyl]benzene-1,2-diol
分子量
Average: 317.3795
Monoisotopic: 317.162708229
CAS号
128470-16-6
ATC分类
C01C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Arbutamine, administered through a closed-loop, computer-controlled drug-delivery system, is indicated to elicit acute cardiovascular responses, similar to those produced by exercise, in order to aid in diagnosing the presence or absence of coronary artery disease in patients who cannot exercise adequately .

生产厂家
  • Gensia automedics inc
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
  • Catecholamines and Derivatives
Substructures
  • Hydroxy Compounds
  • Phenols and Derivatives
  • Catecholamines and Derivatives
  • Benzyl Alcohols and Derivatives
  • Aliphatic and Aryl Amines
  • Benzene and Derivatives
  • Amino Alcohols
  • Catechols
  • Phenethylamines
  • Aromatic compounds
  • Alcohols and Polyols
  • Phenyl Esters
适应症
药理
Indication Used to elicit acute cardiovascular responses (cardiac stumulant), similar to those produced by exercise, in order to aid in diagnosing the presence or absence of coronary artery disease (CAD) in patients who cannot exercise adequately.
Pharmacodynamics Not Available
Mechanism of action Arbutamine is a synthetic catecholamine with positive chronotropic and inotropic properties. The chronotropic (increase in heart rate) and inotropic (increase in force of contraction) effects of arbutamine serve to mimic exercise by increasing cardiac work (producing stress) and provoke myocardial ischemia in patients with compromised coronary arteries. The increase in heart rate caused by arbutamine is thought to limit regional subendocardial perfusion, thereby limiting tissue oxygenation. In functional assays, arbutamine is more selective for beta-adrenergic receptors than for alpha-adrenergic receptors. The beta-agonist activity of arbutamine provides cardiac stress by increasing heart rate, cardiac contractility, and systolic blood pressure. The degree of hypotension that occurs for a given chronotropic activity is less with arbutamine than, for example, with isoproterenol because alpha receptor activity is retained.
Absorption Not Available
Volume of distribution Not Available
Protein binding 58%
Metabolism
Primarily metabolized to methoxyarbutamine. Another possible metabolite is ketoarbutamine. The metabolites of arbutamine appear to have less pharmacological activity and a longer half-life and than the parental drug.

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

Substrate Enzymes Product
Arbutamine
    Ketoarbutamine Details
    Arbutamine
      Methoxyarbutamine Details
      Route of elimination Not Available
      Half life Elimination half-life is approximately 8 minutes.
      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
      logP 2.9 Not Available
      Predicted Properties
      Property Value Source
      water solubility 8.42e-02 g/l ALOGPS
      logP 2.08 ALOGPS
      logP 2 ChemAxon
      logS -3.6 ALOGPS
      pKa (strongest acidic) 8.97 ChemAxon
      pKa (strongest basic) 9.76 ChemAxon
      physiological charge 1 ChemAxon
      hydrogen acceptor count 5 ChemAxon
      hydrogen donor count 5 ChemAxon
      polar surface area 92.95 ChemAxon
      rotatable bond count 8 ChemAxon
      refractivity 89.78 ChemAxon
      polarizability 35.54 ChemAxon
      药物相互作用
      食物相互作用
      Not Available

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