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Identification of a new series of non-peptidic NK3 receptor antagonists |
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| Authors: | Juhl Karsten Hansen Tore Kehler Jan Khanzhin Nikolay A Nørgaard Morten B Ruhland Thomas Larsen Dorrit B Jensen Klaus G Steiniger-Brach Björn Nielsen Søren M Simonsen Klaus B |
| Affiliation: | a Discovery Chemistry and DMPK, H. Lundbeck A/S, Otilliavej 9, DK 2500 Valby, Denmark b Discovery Pharmacology Research, H. Lundbeck, Otilliavej 9, DK 2500 Valby, Denmark |
| 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. |
| Keywords: | NK3 antagonist Schizophrenia Cyclopropane Senktide induced hypoactivity |
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