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Identification of a new series of non-peptidic NK3 receptor antagonists. 2011
Karsten Juhl, and
Tore Hansen, and
Jan Kehler, and
Nikolay A Khanzhin, and
Morten B Nørgaard, and
Thomas Ruhland, and
Dorrit B Larsen, and
Klaus G Jensen, and
Björn Steiniger-Brach, and
Søren M Nielsen, and
Klaus B Simonsen
Discovery Chemistry and DMPK, H. Lundbeck A/S, Valby, Denmark. kaju@lundbeck.com
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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Björn Steiniger-Brach, and
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Klaus G Jensen, and
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Journal of medicinal chemistry,
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September 2013,
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Nikolay A Khanzhin, and
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Klaus G Jensen, and
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September 1995,
Neuroscience letters,
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Thomas Ruhland, and
Dorrit B Larsen, and
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Björn Steiniger-Brach, and
Søren M Nielsen, and
Klaus B Simonsen
March 1994,
European journal of pharmacology,
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Jan Kehler, and
Nikolay A Khanzhin, and
Morten B Nørgaard, and
Thomas Ruhland, and
Dorrit B Larsen, and
Klaus G Jensen, and
Björn Steiniger-Brach, and
Søren M Nielsen, and
Klaus B Simonsen
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Cardiovascular & hematological agents in medicinal chemistry,
