Identification of a new series of non-peptidic NK<sub>3sub> receptor antagonists
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- 作者：Karsten Juhl<sup>asup><sup> ; sup><sup>kaju@lundbeck.comsup> ; Tore Hansen<sup>asup><sup> ; sup><sup>† ; sup> ; Jan Kehler<sup>asup> ; Nikolay A. Khanzhin<sup>asup> ; Morten B. Nø ; rgaard<sup>asup> ; Thomas Ruhland<sup>asup> ; Dorrit B. Larsen<sup>asup> ; Klaus G. Jensen<sup>asup> ; Bjö ; rn Steiniger-Brach<sup>bsup> ; Sø ; ren M. Nielsen<sup>bsup> ; Klaus B. Simonsen<sup>asup>
- 关键词：NK<sub>3sub> antagonist ; Schizophrenia ; Cyclopropane ; Senktide induced hypoactivity
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2011
- 出版时间：1 March 2011
- 年：2011
- 卷：21
- 期：5
- 页码：1498-1501
- 全文大小：1352 K
文摘
The identification and structure–activity relationships of 2-aminomethyl-1-aryl cyclopropane carboxamides as novel NK<sub>3sub> receptor antagonists are reported. The compound series was optimized to give analogues with low nanomolar binding to the NK<sub>3sub> receptor and brain exposure, leading to activity in vivo in the senktide-induced hypoactivity model in gerbils.