1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists

Abstract The structure–activity relationships of novel 1,5-benzodioxepin derivatives as muscarinic M 1 –M 3 receptor antagonists are reported. Some of these compounds were found to possess high binding affinity for the muscarinic M 3 receptor and potent effect on rhythmic increase in bladder pressure in unanesthetized rats following oral administration. These compounds displayed selectivity for the bladder over the salivary gland.