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This video describes the discovery of nivasorexant, a selective orexin-1 receptor antagonists for the treatment of obsessive compulsive disorders. The content of this video was reported by scientists of Idorsia Pharmaceuticals in Allschwil, Switzerland as a Drug Annotation article in the Journal of Medicinal Chemistry. The discovery project started with an advanced compound from previous research, a dual orexin receptor antagonist with poor selectivity between OX1 and OX2. Selectivity for OX1 was refined through improved understanding of the SAR of the series. Research culminated in a compound that was orally available with good brain exposure and efficacy in a rat model for behavioral disorders. Nivasorexant completed phase I trials but failed to meet its primary endpoint in a phase II trial for eating disorders.
This video was created for academic purposes. The creator of the video has no financial stake in the sponsor of the research described in this video.
Негізгі бет discovery of nivasorexant, an orexin-1 receptor antagonist
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