Formoterol (hemifumarate hydrate)

Formoterol is a selective agonist of the β₂-adrenergic receptor (β₂-AR; K_is = 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)