Salmeterol is a potent and selective β2-AR adrenoceptor agonist (EC50 = 5.3 nM) that displays bronchodilator actions. Unlike other β2-AR agonists, Salmeterol binds to exo-site domain of β2-AR receptors, producing a slow onset of action and prolonged activation.
Johnson et al (1993) The pharmacology of salmeterol. Life Sci. 52 2131. Ellis et al (1995) Correlation of cyclic AMP accumulation and relaxant actions of salmeterol and salbutamol in bovine tracheal smooth muscle. Br.J.Pharmacol. 116 2510. Clark et al (1996) Stable activation and desensitization of beta 2-adrenergic receptor stimulation of adenylyl cyclase by salmeterol: evidence for quasi-irreversible binding to an exosite. Mol.Pharmacol. 49 182.
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Manoharan et alManoharan et al. (PubMed ID 2620533) used salmeterol, a potent and selective 2-AR agonist, to treat persistent asthma and found it to improve impulse oscillometry. -SCBT Publication Review
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