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A Tissue-Selective Nonsteroidal Progesterone Receptor Modulator: 7,9-Difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochro meno[3,4-f]quinoline.

  作者 Pedram, Bijan;van Oeveren, Arjan;Mais, Dale E.;Marschke, Keith B.;Verbost, Pieter M.;Groen, Marinus B.;Zhi, Lin;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-13;  页码  3696-3699  
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[摘要]The progesterone receptor plays an important role in the female reproductive system. Here the authors describe the discovery of a new selective progesterone receptor modulator (SPRM). In rats, the lead compd. (I), inhibited ovulation and showed full efficacy in uterine and vaginal tissue but was a mixed partial agonist/antagonist in breast tissue. The compd. also suppressed ovulation in monkeys, but in contrast to currently approved steroidal PR agonists, it did not suppress estradiol levels.

 
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