Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8 , CYP2C9 , CYP2C19 and CYP3A4 ( IC 50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder.
Products | Products > Disease Areas > Neurological, Eye or Ear Disease | Products > Signaling Pathways > GPCR/G Protein | Products > Signaling Pathways > Neuronal Signaling | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Neurological Disease | Products > Signaling Pathways > Orexin Receptor (OX Receptor) | Products > Signaling Pathways > Cytochrome P450
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