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

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 un...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-02, Vol.17 (4), p.925-931
Hauptverfasser:	SONDA, Shuji, KATAYAMA, Kenichi, FUJIO, Masakazu, SAKASHITA, Hiroshi, INABA, Kenichi, ASANO, Kiyoshi, AKIRA, Toshiaki
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding, Competitive - drug effects Biological and medical sciences Cell Line Cholinergic system Humans Indicators and Reagents Insecta Mandelic Acids - pharmacology Medical sciences Muscarinic Antagonists - chemical synthesis Muscarinic Antagonists - metabolism Muscarinic Antagonists - pharmacology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Oxepins - chemical synthesis Oxepins - metabolism Oxepins - pharmacology Pharmacology. Drug treatments Rats Receptor, Muscarinic M3 - antagonists & inhibitors Salivary Glands - drug effects Scopolamine Hydrobromide - metabolism Structure-Activity Relationship Urinary Bladder, Neurogenic - drug therapy Urinary system
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.11.058