Salmeterol(GR 33343X) xinafoate is a long-acting beta2-adrenergic receptor agonist drug that is prescribed for the treatment of asthma and chronic obstructive pulmonary disease(COPD).
IC50 Value: 1.5±0.4 nM (Ki value for Wtβ2 AR)
Target: beta2-adrenergic receptor
 It is available as a dry powder inhaler that releases a powdered form of the drug.
in vitro: Treatment with the selective beta-2-adrenergic receptor agonist, salmeterol, significantly decreased phosphorylation of IRS-1(Ser307). Following IRS-1 shRNA transfection+salmeterol treatment, Bcl-2-associated X protein (Bax) and cytochrome c levels were significantly decreased.
in vivo: Salmeterol was significantly better than disodium cromoglycate in improving both morning (mean difference between treatments = 31 L/min; P = .007) and evening PEF (mean difference between treatments = 29 L/min; P = .008). Both treatments were however, associated with significant improvement in FEV1, daytime and night-time symptoms score and use of rescue salbutamol (P < .001). Salmeterol decreases the production of pro-inflammatory cytokines in a model of allergen-challenged mice that expressed tumor-necrosis factor-alpha, interleukin-1 and interleukin-6.
Clinical trial: Dose-Ranging Study of the Salmeterol Component of Fluticasone/Salmeterol Spiromax Compared to Fluticasone Spiromax and Advair Diskus in Asthma Subjects. Phase 2

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