title: 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.
authors.affiliation: Process Chemistry Laboratories, Pharmaceutical Technology Center, Mitsubishi Pharma Corporation, 14, Sunayama, Kamisu, Ibaraki 314-0255, Japan. Sonda.Shuuji@ma.m-pharma.co.jp
authors.forename: Shuji
authors.initials: S
authors.lastname: Sonda
authors.forename: Kenichi
authors.initials: K
authors.lastname: Katayama
authors.forename: Masakazu
authors.initials: M
authors.lastname: Fujio
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Sakashita
authors.forename: Kenichi
authors.initials: K
authors.lastname: Inaba
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Asano
authors.forename: Toshiaki
authors.initials: T
authors.lastname: Akira
mesh_terms: D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002460:Cell Line; D006801:Humans; D007202:Indicators and Reagents; D007313:Insecta; D008333:Mandelic Acids / Q000494:pharmacology; D018727:Muscarinic Antagonists / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D010082:Oxepins / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D043587:Receptor, Muscarinic M3 / Q000037:antagonists & inhibitors*; D012469:Salivary Glands / Q000187:drug effects; D012601:Scopolamine / Q000378:metabolism; D013329:Structure-Activity Relationship; D001750:Urinary Bladder, Neurogenic / Q000188:drug therapy
chemical_list: D007202:Indicators and Reagents; D008333:Mandelic Acids; D018727:Muscarinic Antagonists; D010082:Oxepins; D043587:Receptor, Muscarinic M3; D012601:Scopolamine; C005419:oxybutynin