Identification of a new series of non-peptidic NK3 receptor antagonists.

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

Bioorganic & Medicinal Chemistry Letters（2011）

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摘要

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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关键词

NK3 antagonist,Schizophrenia,Cyclopropane,Senktide induced hypoactivity

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