Description
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.
Description
Salmeterol is a long-acting β
2-adrenergic receptor agonist (β
2-AR; EC
50s = 0.79, 63.1, and 9.4 nM for β
2-, β
1-, and β
3-ARs, respectively). It inhibits electrically-stimulated contraction of isolated guinea pig trachea strips (EC
50 = 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 β
2-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.
Chemical Properties
White to Off-White Solid
Originator
Glaxo (United Kingdom)
Uses
Bronchodilator; Beta2-adrenoceptor agonist
Uses
Smooth wheezing anti-inflammatory
Uses
A β2-Adrenergic agonist. Structural analog of Albuterol (A514500).
Uses
A ?-Adrenergic agonist. Structural analog of albuterol
Application
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).
Definition
ChEBI: Salmeterol xinafoate is a naphthoic acid.
brand name
Serevent (GlaxoSmithKline).
Biochem/physiol Actions
β2-adrenoceptor agonist.
