| Literature DB >> 25978072 |
Masahiro Eda, Tomoko Kuroda, Satoshi Kaneko, Yoshiyuki Aoki, Masami Yamashita, Chieko Okumura, Yoshitaka Ikeda, Tomoko Ohbora, Masaki Sakaue, Natsumi Koyama, Keiichi Aritomo.
Abstract
The steroidal glucocorticoid antagonist mifepristone has been reported to improve the symptoms of depression. We report the discovery of 6-(3,5-dimethylisoxazol-4-yl)-2,2,4,4-tetramethyl-2,3,4,7,8,9-hexahydro-1H-cyclopenta[h]quinolin-3-one 3d (QCA-1093) as a novel nonsteroidal glucocorticoid receptor antagonist. The compound displayed potent in vitro activity, high selectivity over other steroid hormone receptors, and significant antidepressant-like activity in vivo.Entities:
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Year: 2015 PMID： 25978072 DOI： 10.1021/jm501758q
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446