The identification and structure activity relationships of isoquinolinone-4-carboxamides as novel NK3 receptor antagonists are presented. The compound series was optimized to give compounds that show antipsychotic potential  in the amphetamine induced hyperactivity model in guinea pigs.SAR on NK3/NK2 selectivity, brain/plasma ratios and in vivo binding to the NK3 receptor in guinea pigs are discussed.

Isoquinolinone-4-carboxamides as NK3 receptor antagonists: Discovery of development candidate Lu AE61035

246th National Meeting (2013)

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