Drug intelligence / Profile preview

albuterol + phentolamine

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Inhalation
01

Overview

Albuterol + phentolamine is an experimental combination of two small molecule drugs used in research for respiratory conditions such as asthma. Albuterol (also known as salbutamol) is a selective beta-2 adrenergic receptor agonist that acts as a bronchodilator by relaxing airway smooth muscle, leading to improved airflow. Phentolamine is a reversible, competitive antagonist at alpha-1 and alpha-2 adrenergic receptors; it causes vasodilation of vascular smooth muscle and can influence bronchial tone through its effects on the autonomic nervous system. In clinical studies, the combination has been shown to produce greater bronchodilation than either agent alone in some patients with asthma, though results are variable[1]. The mechanism involves simultaneous stimulation of beta-2 receptors (albuterol) to relax bronchial muscles and blockade of alpha receptors (phentolamine), which may further reduce bronchoconstriction[1][2][7].

Other names
albuterol and phentolaminesalbutamol and phentolamine
02

Targets

ADRA1A (α1A)ADRB2 (β2)ADRA2A (α2A)

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