Literature DB >> 17188867

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

Shuji Sonda1, Kenichi Katayama, Masakazu Fujio, Hiroshi Sakashita, Kenichi Inaba, Kiyoshi Asano, Toshiaki Akira.   

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.

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Year:  2006        PMID: 17188867     DOI: 10.1016/j.bmcl.2006.11.058

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.

Authors:  Aaron M Bender; Rebecca L Weiner; Vincent B Luscombe; Hyekyung P Cho; Colleen M Niswender; Darren W Engers; Thomas M Bridges; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2017-04-04       Impact factor: 2.823

  1 in total

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