Formoterol (hemifumarate hydrate)

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.1,2 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.4,5,6WARNING This product is not for human or veterinary use.

[1] ANDERSON G P. Formoterol: Pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective β2-adrenoceptor agonist bronchodilator[J]. Life sciences, 1993, 52 26: Pages 2145-2160. DOI: 10.1016/0024-3205(93)90729-m
[2] N. DECKER. Effects of N-aralkyl substitution of β-agonists on α- and β-adrenoceptor subtypes: pharmacological studies and binding assays[J]. Journal of Pharmacy and Pharmacology, 1982, 34 2: 107-112. DOI: 10.1111/j.2042-7158.1982.tb04195.x
[3] HARUHITO SUGIYAMA MD. The effect of formoterol on the late asthmatic phenomena in guinea pigs[J]. Journal of Allergy and Clinical Immunology, 1992, 89 4: Pages 858-866. DOI: 10.1016/0091-6749(92)90442-5
[4] MARC L DECRAMER. The safety of long-acting β2-agonists in the treatment of stable chronic obstructive pulmonary disease.[J]. International Journal of Chronic Obstructive Pulmonary Disease, 2013, 8: 53-64. DOI: 10.2147/copd.s39018
[5] DONALD P TASHKIN  Gary T F. Combination bronchodilator therapy in the management of chronic obstructive pulmonary disease.[J]. Respiratory Research, 2013, 14: 49. DOI: 10.1186/1465-9921-14-49
[6] ADRIANA YOCK CORRALES  Mike S  Manuel Soto Martinez. Management of severe asthma in children.[J]. Australian family physician, 2011, 40 1-2: 35-38.