Procaterol is an agonist of β
2-adrenergic receptors (β
2-ARs).
1 It binds to (K
d = 46 pM), and is selective for, β
2-ARs over β
1-ARs (K
d = 4,000 pM). Procaterol binds more potently to β
2-ARs in isolated guinea pig lung than to β
1-ARs in isolated guinea pig cardiac ventricle in the presence (IC
50s = 175 and 1,660 nM, respectively) and absence of GTP (Item No.
16060; IC
50s = 55.1 and 1,660 nM, respectively).
2 It inhibits contractions induced by acetylcholine (Item No.
23829) in isolated guinea pig trachea (EC
50 = 10.5 nM).
3 In vivo, procaterol inhibits histamine-induced airflow obstruction in a guinea pig model of ovalbumin-sensitized asthma when administered
via inhalation at a dose of 10 μg/ml.
4 
