Salmeterol-d3 is intended for use as an internal standard for the quantification of salmeterol by GC- or LC-MS. 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).1 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.2 Salmeterol binds to an exosite domain of β2-adrenergic receptors, producing a slow onset of action and prolonged activation.3 Formulations containing salmeterol have been used in the treatment of asthma, including exercise-induced asthma, and chronic obstructive pulmonary disease.
1.Procopiou, P.A., Barrett, V.J., Ford, A.J., et al.The discovery of long-acting saligenin β2 adrenergic receptor agonists incorporating a urea groupBioorg. Med. Chem.19(20)6026-6032(2011) 2.Ball, D.I., Brittain, R.T., Coleman, R.A., et al.Salmeterol, a novel, long-acting β2-adrenoceptor agonist: Characterization of pharmacological activity in vitro and in vivoBr. J. Pharmacol.104(3)665-671(1991) 3.Isin, B., Estiu, G., Wiest, O., et al.Identifying ligand binding conformations of the β2-adrenergic receptor by using its agonists as computational probesPLoS One7(12)e50186(2012)