Formoterol-13C-d3 is intended for use as an internal standard for the quantification of formoterol by GC- or LC-MS. Formoterol is a selective agonist of the β2-adrenergic receptor (β2-AR; Kis = 7.58 and 2,630 nM for β2- and β1-ARs, respectively).1 It is selective for β-ARs in isolated guinea pig trachea over those in atrial tissue (pD2s = 9.29 and 6.98, respectively) and has a long duration of action.2,1 Aerosolized formoterol (10 µg/ml, inhaled) prevents the late asthmatic response and eosinophil and macrophage infiltration in bronchoalveolar lavage fluid (BALF), and as well as reduces bronchial reactivity in a guinea pig model of allergic asthma induced by ovalbumin.3 Formulations containing formoterol have been used, alone and in combination with other compounds, in the treatment of chronic obstructive pulmonary disease and asthma.4,5,6
1.Anderson, G.P.Formoterol: Pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective β2-adrenoceptor agonist bronchodilatorLife Sciences52(26)2145-2160(1993) 2.Decker, N., Quennedey, M.C., Rouot, B., et al.Effects of N-aralkyl substitution of β-agonists on α- and β-adrenoceptor subtypes: Pharmacological studies and binding assaysJ. Pharm. Pharmacol.34(2)107-112(1982) 3.Sugiyama, H., Okada, C., Bewtra, A.K., et al.The effect of formoterol on the late asthmatic phenomena in guinea pigsJ. Allergy Clin. Immunol.89(4)858-866(1992) 4.Decramer, M.L., Hanania, N.A., LÖtvall, J.O., et al.The safety of long-acting β2-agonists in the treatment of stable chronic obstructive pulmonary diseaseInt. J. Chron. Obstruct. Pulmon. Dis.853-64(2013) 5.Tashkin, D.P., and Ferguson, G.T.Combination bronchodilator therapy in the management of chronic obstructive pulmonary diseaseRespir. Res.14(1)49(2013) 6.Bush, A., and Saglani, S.Management of severe asthma in childrenLancet376(9743)814-825(2010)