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Aformoterol is the (R,R)-enantiomer of the β2-adrenergic receptor (β2-AR) agonist formoterol (Item No. 15584).1 It selectively binds to β1- over β2-ARs (Kds = 2.9 and 113 nM, respectively) as well as β3-adrenergic, B2 bradykinin, neurokinin 1 (NK1) and NK2 receptors when used at concentrations up to 3 μM. Aformoterol induces cAMP accumulation in cultured human bronchial epithelial cells. Ex vivo, aformoterol (0.01-1,000 nM) induces dose-dependent relaxation of guinea pig tracheal strips precontracted with carbamoylcholine (Item No. 14486), ovalbumin, or histamine (pD2s = 8.4, 9.5, and 9.5, respectively). In vivo, aformoterol reverses histamine- and ovalbumin-induced bronchoconstriction in guinea pigs (ED50s = 1 and 40 nmol/kg, respectively). Formulations containing aformoterol have been used in the treatment of chronic obstructive pulmonary disease (COPD).
WARNING This product is not for human or veterinary use.
1. Biological actions of formoterol isomers. Pulm. Pharmacol. Ther. 15(2), 135-145 (2002).