(R)-Bambuterol is a β2-receptor agonist with anti-asthmatic and colitis-improving activity. (R)-Bambuterol is indicated for the treatment of asthma and chronic obstructive pulmonary disease and has the advantage of a once-daily dosing and a favorable side effect profile. (R)-Bambuterol significantly reduced disease severity in a mouse model of colitis, more effectively than (RS)-Bambuterol or (S)-Bambuterol. (R)-Bambuterol can significantly reduce the levels of inflammatory cytokines and reduce the infiltration of macrophages in mice with colitis. (R)-Bambuterol also increases β2-adrenoceptor levels and reduces the expression of IL-6 , IL-17 and other related proteins in colon tissue in a dose-dependent manner.