Peer-reviewed veterinary case report
Identification of a new series of non-peptidic NK3 receptor antagonists.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2011
- Authors:
- Juhl, Karsten et al.
- Affiliation:
- Discovery Chemistry and DMPK
- Species:
- rodent
Abstract
The identification and structure-activity relationships of 2-aminomethyl-1-aryl cyclopropane carboxamides as novel NK(3) receptor antagonists are reported. The compound series was optimized to give analogues with low nanomolar binding to the NK(3) receptor and brain exposure, leading to activity in vivo in the senktide-induced hypoactivity model in gerbils.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/21292483/