Salmeterol hydroxynaphthoate is a new long-acting β2-selective adrenoceptor agonist
introduced as a bronchodilator for the treatment of reversible airway obstruction in asthma
and chronic bronchitis. It has bronchodilatory activity as intense and four times longerlasting
than equivalent doses of salbutamol. Salmeterol hydroxynaphthoate is reported to
be the first bronchodilator with significant anti-inflammatory activity and hence could
complement prophylactic corticosteroid therapy.
Salmeterol is a long-acting β2-adrenergic receptor agonist (β2-AR; EC50s = 0.79, 63.1, and 9.4 nM for β2-, β1-, and β3-ARs, respectively). It inhibits electrically-stimulated contraction of isolated guinea pig trachea strips (EC50 = 2.51 nM) and histamine-induced bronchoconstriction in guinea pigs via aerosol administration of doses ranging from 0.12 to 12 mM. Salmeterol binds to an exosite domain of β2-adrenergic receptors, producing a slow onset of action and prolonged activation. Formulations containing salmeterol have been used in the treatment of asthma, including exercise-induced asthma, and chronic obstructive pulmonary disease.
Bronchodilator; Beta2-adrenoceptor agonist
Smooth wheezing anti-inflammatory
A β2-Adrenergic agonist. Structural analog of Albuterol (A514500).
A -Adrenergic agonist. Structural analog of albuterol
Salmeterol xinafoate is a potent and selective β2-adrenoceptor agonist (EC50 = 5.3 nM) that displays bronchodilator actions. Unlike other β2- adrenoceptor agonists, Salmeterol binds to exo-site domain of β2-AR receptors, producing a slow onset of action and prolonged activation. Clinically used for the treatment of asthma and chronic obstructive pulmonary disease(COPD).
ChEBI: Salmeterol xinafoate is a naphthoic acid.
Serevent (GlaxoSmithKline).
[1] PANAYIOTIS A. PROCOPIOU . The discovery of long-acting saligenin β2 adrenergic receptor agonists incorporating a urea group[J]. Bioorganic & Medicinal Chemistry, 2011, 19 20: Pages 6026-6032. DOI:
10.1016/j.bmc.2011.08.043[2] D.I. BALL. Salmeterol, a novel, long-acting β2-adrenoceptor agonist: characterization of pharmacological activity in vitro and in vivo[J]. British Journal of Pharmacology, 1991, 104 3: 665-671. DOI:
10.1111/j.1476-5381.1991.tb12486.x[3] BASAK ISIN. Identifying ligand binding conformations of the β2-adrenergic receptor by using its agonists as computational probes.[J]. ACS Applied Bio Materials, 2012: e50186. DOI:
10.1371/journal.pone.0050186
