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 |
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| container_end_page | 931 |
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| container_issue | 4 |
| container_start_page | 925 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 17 |
| creator | SONDA, Shuji KATAYAMA, Kenichi FUJIO, Masakazu SAKASHITA, Hiroshi INABA, Kenichi ASANO, Kiyoshi AKIRA, Toshiaki |
| description | 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. |
| doi_str_mv | 10.1016/j.bmcl.2006.11.058 |
| format | Article |
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Drug treatments</subject><subject>Rats</subject><subject>Receptor, Muscarinic M3 - antagonists & inhibitors</subject><subject>Salivary Glands - drug effects</subject><subject>Scopolamine Hydrobromide - metabolism</subject><subject>Structure-Activity Relationship</subject><subject>Urinary Bladder, Neurogenic - drug therapy</subject><subject>Urinary system</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkMFq3DAURUVI6UyT_kAWRZt0VTt6sizLyzS0TSAlmwS6E7L0VDTY1kSyhzRfXw8zMPDgvsW5d3EIuQJWAgN5sym7wfYlZ0yWACWr1RlZg5CiqASrz8matZIVqhV_VuRTzhvGQDAhPpIVNKCUks2aPMO3uviO43t0Ib7hNozUYQo7M4UdZmqWo2PcYU9tb3Km0dNhztakMAZLf1c0ocXtFBM142T-xjHkKV-SD970GT8f84K8_PzxfHdfPD79eri7fSwsF3IqDHZgW9u5TjXeVMw1yyc79MLJlhvJna-xBSO886xDI5SFqvW-UdyBq3h1Qb4edrcpvs6YJz2EbLHvzYhxzlqqtoGWNwvID6BNMeeEXm9TGEz6p4HpvUu90XuXeu9SA-jF5VL6clyfuwHdqXKUtwDXR8AsRnqfzGhDPnGqrlgjePUfPtV_mQ</recordid><startdate>20070215</startdate><enddate>20070215</enddate><creator>SONDA, Shuji</creator><creator>KATAYAMA, Kenichi</creator><creator>FUJIO, Masakazu</creator><creator>SAKASHITA, Hiroshi</creator><creator>INABA, Kenichi</creator><creator>ASANO, Kiyoshi</creator><creator>AKIRA, Toshiaki</creator><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20070215</creationdate><title>1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists</title><author>SONDA, Shuji ; KATAYAMA, Kenichi ; FUJIO, Masakazu ; SAKASHITA, Hiroshi ; INABA, Kenichi ; ASANO, Kiyoshi ; AKIRA, Toshiaki</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c246t-aeb1c9cbdb87fa30d7db86bef4d692a62df5e91a4fdf0bea48c139ff782d1d323</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Animals</topic><topic>Binding, Competitive - drug effects</topic><topic>Biological and medical sciences</topic><topic>Cell Line</topic><topic>Cholinergic system</topic><topic>Humans</topic><topic>Indicators and Reagents</topic><topic>Insecta</topic><topic>Mandelic Acids - pharmacology</topic><topic>Medical sciences</topic><topic>Muscarinic Antagonists - chemical synthesis</topic><topic>Muscarinic Antagonists - metabolism</topic><topic>Muscarinic Antagonists - pharmacology</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. 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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2007-02, Vol.17 (4), p.925-931 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | 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 |
| title | 1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists |
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