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药品详细

Tolazoline(妥拉苏林)

化学结构式图
中文名
妥拉苏林
英文名
Tolazoline
分子式
C10H12N2
化学名
2-benzyl-4,5-dihydro-1H-imidazole
分子量
Average: 160.2157
Monoisotopic: 160.100048394
CAS号
59-98-3
ATC分类
C04A 未知;M02A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A vasodilator that apparently has direct actions on blood vessels and also increases cardiac output. Tolazoline can interact to some degree with histamine, adrenergic, and cholinergic receptors, but the mechanisms of its therapeutic effects are not clear. It is used in treatment of persistent pulmonary hypertension of the newborn. [PubChem]

生产厂家
  • Novartis pharmaceuticals corp
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
  • Phenethylamines
Substructures
  • Imidazolines
  • Carboxylic Acids and Derivatives
  • Benzene and Derivatives
  • Imidazoles
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamidines
  • Imines
适应症
药理
Indication For the treatment of pulmonary artery anomalies
Pharmacodynamics Tolazoline is a pulmonary vasodilator indicated used to decrease pulmonary vascular resistance (PVR) in persistent pulmonary hypertension of the newborn (PPHN).
Mechanism of action Vasodilation by means of a direct effect on peripheral vascular smooth muscle and indirect effects produced, in part, by release of endogenous histamine; tolazoline has moderate alpha-adrenergic blocking activity and has histamine agonist activity. Tolazoline usually reduces pulmonary arterial pressure and vascular resistance.
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 174 °C PhysProp
water solubility 373 mg/L Not Available
logP 2.65 SANGSTER (1993)
pKa 10.3 SANGSTER (1994)
Predicted Properties
Property Value Source
water solubility 1.36e+00 g/l ALOGPS
logP 2.05 ALOGPS
logP 1.2 ChemAxon
logS -2.1 ALOGPS
pKa (strongest basic) 10.25 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 24.39 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 49.07 ChemAxon
polarizability 17.94 ChemAxon
药物相互作用
Drug Interaction
Cimetidine Anticipated loss of efficacy of tolazoline
Ranitidine Anticipated loss of efficacy of tolazoline
Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
食物相互作用
Not Available

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