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The standard treatment for chronic obstructive pulmonary disease is a combination of anti-inflammatory drugs and bronchodilators. We recently found that mepenzolate bromide ( MP ), an antagonist for human muscarinic M3 receptor (hM 3 R), has both anti-inflammatory and short-acting bronchodilatory activities. To obtain  MP  derivatives with longer-lasting bronchodilatory activity, we synthesized hybrid compounds based on  MP  and two other muscarinic antagonists with long-acting bronchodilatory activity glycopyrronium bromide ( GC ) and aclidinium bromide ( AD ). Of these three synthesized hybrid compounds ( MP-GC, GC-MP, MP-AD ) and  MP, MP-AD  showed the highest affinity for hM 3 R and had the longest lasting bronchodilatory activity, which was equivalent to that of  GC  and  AD . Both  MP-GC  and  MP-AD  exhibited an anti-inflammatory effect equivalent to that of MP, whereas, in line with  GC  and  AD, GC-MP  did not show this effect. We also confirmed that administration of  MP-AD  suppressed elastase-induced pulmonary emphysema in a mouse model. These findings provide important information about the structure-activity relationship of  MP  for both bronchodilatory and anti-inflammatory activities.

Identification of Mepenzolate Derivatives With Long-Acting Bronchodilatory Activity