Novel N-acyl-carbazole derivatives as 5-HT7R antagonists
详细信息 查看全文
- 作者：Youngjae Kima ; b ; Miyoung Yeoma ; Jinsung Taeb ; Hyewhon Rhimc ; d ; Hyunah Chooa ; e ; hchoo@kist.re.kr" class="auth_mail" title="E-mail the corresponding author
- 关键词：5-HT7R ; Antagonist ; N-Acyl-carbazole ; Serotonin ; Depression ; GPCR
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：3 March 2016
- 年：2016
- 卷：110
- 期：Complete
- 页码：302-310
- 全文大小：1262 K
文摘
- •
Discovery of novel N-acyl-carbazoles as 5-HT7R antagonists.
- •
5">Potent binding affinity against 5-HT7R (IC50 = 74 nM).
- •
Selectivities over other serotonin receptor subtypes, and hERG channel.
- •
5">Good pharmacokinetic profile with oral bioavailability (F 67.8%).
- •
Good antidepressant effect in in vivo animal study.