Preville, Cathy published the artcileSubstituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793, Recommanded Product: 2-Chloro-5-(trifluoromethyl)pyrazine, the main research area is orexin OX1 OX2 SORA1 neuropeptides bioavailable brain OX1R antagonists.
The orexin system consists of two neuropeptides (orexin-A and orexin-B) that exert their mode of action on two receptors (orexin-1 and orexin-2). While the role of the orexin-2 receptor is established as an important modulator of sleep wake states, the role of the orexin-1 receptor is believed to play a role in addiction, panic, or anxiety. In this manuscript, we describe the optimization of a nonselective substituted azabicyclo[2.2.1]heptane dual orexin receptor antagonist (DORA) into orally bioavailable, brain penetrating, selective orexin-1 receptor (OX1R) antagonists. This resulted in the discovery of our first candidate for clin. development, JNJ-54717793.
ACS Medicinal Chemistry Letters published new progress about Bioavailability (orally bioavailable). 799557-87-2 belongs to class pyrazines, name is 2-Chloro-5-(trifluoromethyl)pyrazine, and the molecular formula is C5H2ClF3N2, Recommanded Product: 2-Chloro-5-(trifluoromethyl)pyrazine.