Salmeterol-d₃

Salmeterol-d₃ is intended for use as an internal standard for the quantification of salmeterol (Item No. 16009) 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.

WARNING This product is not for human or veterinary use.

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 group. Bioorg. 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 vivo. Br. 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 probes. PLoS One 7(12), e50186 (2012).