A long-acting β2-AR agonist
Tulobuterol is a long-acting agonist of the β2-adrenergic receptor (β2-AR).1 It binds to the bovine skeletal muscle β2-AR (Kd = 0.13 ?M). Transdermal administration of tulobuterol (6 and 12 mg/kg) decreases total leukocyte infiltration into the bronchoalveolar lavage fluid (BALF) in a mouse model of allergic asthma induced by ovalbumin.2 It also inhibits rhinovirus replication in infected primary human tracheal epithelial cells when used at a concentration of 0.1 ?M, an effect that can be reversed by the β2-AR antagonist ICI 118551 .3 Formulations containing tulobuterol have been used in the treatment of asthma.
1.IJzerman, A.P., Bultsma, T., and Timmerman, H.Quantitative evaluation of the β2-adrenoceptor intrinsic activity of N-tert-butylphenylethanolaminesJ. Med. Chem.29(4)549-554(1986) 2.Fu, L., Guan, J., Zhang, Y., et al.Tulobuterol patch alleviates allergic asthmic inflammation by blockade of Syk and NF-κB activation in miceOncotarget9(15)12154-12163(2018) 3.Yamaya, M., Nishimura, H., Nadine, L., et al.Tulobuterol inhibits rhinovirus infection in primary cultures of human tracheal epithelial cellsPhysiol. Rep.1(3)e00041(2013)
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