62929-91-3

Procaterol is an agonist of β₂-adrenergic receptors (β₂-ARs). It binds to (K_d = 46 pM), and is selective for, β₂-ARs over β₁-ARs (K_d = 4,000 pM). Procaterol binds more potently to β₂-ARs in isolated guinea pig lung than to β₁-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; IC₅₀s = 55.1 and 1,660 nM, respectively). It inhibits contractions induced by acetylcholine (Item No. 23829) in isolated guinea pig trachea (EC₅₀ = 10.5 nM). 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.

adrenergic agonists

Specific and very potent β 2 agonist.

β2-adrenoceptor agonist; bronchodilator.

Store at RT

[1] S MARULLO. Selective binding of ligands to beta 1, beta 2 or chimeric beta 1/beta 2-adrenergic receptors involves multiple subsites.[J]. EMBO Journal, 1990, 9 5: 1471-1476. DOI: 10.1002/j.1460-2075.1990.tb08264.x
[2] HIDEO KIKKAWA  Katsuo I  Kazuaki Naito. Tracheal Relaxing Effects and β2-Selectivity of TA-2005, a Newly Developed Bronchodilating Agent, in Isolated Guinea Pig Tissues[J]. Japanese journal of pharmacology, 1991, 57 2: Pages 175-185. DOI: 10.1254/jjp.57.175
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[4] MIRZA. Inhaled procaterol inhibits histamine-induced airflow obstruction and microvascular leakage in guinea-pig airways with allergic inflammation[J]. Clinical and Experimental Allergy, 2008, 28 5: 644-652. DOI: 10.1046/j.1365-2222.1998.00263.x