Byline: Shui-Juan Zhang, Jun-Xia Jiang, Qian-Qian Ren, Qiang-Min Xie, Yao-Kang Xiong Keywords: bencycloquidium bromide; drug delivery; muscarinic receptor antagonist; cigarette smoke; airway inflammation ABSTRACT Preclinical Research Bencycloquidium bromide (BCQB), a novel M.sub.3 receptor antagonist, alleviates airway hyperresponsiveness, inflammation, and airway remodeling in a murine model of asthma. The aim of this study was to investigate the anti-inflammatory activity of inhaled BCQB in a cigarette smoke (CS)-induced model of acute lung inflammation. Mice exposed to CS developed chronic obstructive pulmonary disease (COPD). Inhalation of BCQB suppressed the accumulation of neutrophils and macrophages in airways and lung and also inhibited the CS-induced increases in mRNA levels of keratinocyte-derived chemokine, monocyte chemotactic protein-1, tumor necrosis factor-alpha, and interleukin-1[beta] in lung and protein expression levels in bronchoalveolar lavage fluid. Moreover, BCQB (300 I1/4g/ml) inhibited the CS-induced changes in superoxide dismutase and myeloperoxidase activities in the lungs. Our study suggests that BCQB might be a potential therapy for inflammation in CS-induced pulmonary diseases, including COPD. Drug Dev Res 73 : 123-131, 2015. [c] 2015 Wiley Periodicals, Inc.