Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373174 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
The identification and structure–activity relationships of 2-aminomethyl-1-aryl cyclopropane carboxamides as novel NK3 receptor antagonists are reported. The compound series was optimized to give analogues with low nanomolar binding to the NK3 receptor and brain exposure, leading to activity in vivo in the senktide-induced hypoactivity model in gerbils.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Karsten Juhl, Tore Hansen, Jan Kehler, Nikolay A. Khanzhin, Morten B. Nørgaard, Thomas Ruhland, Dorrit B. Larsen, Klaus G. Jensen, Björn Steiniger-Brach, Søren M. Nielsen, Klaus B. Simonsen,