TAK-925, an orexin 2 receptor-selective agonist, shows robust wake-promoting effects in mice

• Published in: Pharmacology, biochemistry and behavior Vol. 187; p. 172794
• Main Authors: Yukitake, Hiroshi, Fujimoto, Tatsuhiko, Ishikawa, Takashi, Suzuki, Atsushi, Shimizu, Yuji, Rikimaru, Kentaro, Ito, Mitsuhiro, Suzuki, Motohisa, Kimura, Haruhide
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.12.2019
• Subjects: Hypersomnia; Narcolepsy; Orexin; Orexin 2 receptor; Orexin 2 receptor agonist; TAK-925; BBB; DMSO; CHO; BSA; EDS; FBS; IC50; Orexin 2 receptor agonist; EC50; qPCR; EMG; EEG; NT1; OX2R; ROI; ssODN; GPCR; ZT; ERK; TAK-925; Hypersomnia; NREM; Orexin 2 receptor; OX1R; PPN; SC; CREB; CSF; HDR; TTX; Narcolepsy; VLP; WT; Orexin; HTRF; KO; h; ACSF; IP1; EDTA; TMN; HEPES; LC; OX-A; SCH; HBSS; OX-B; REM; ICV

Orexin-producing neurons in the lateral hypothalamus are a critical regulator of sleep/wake states, and their loss is associated with narcolepsy type 1 (NT1). Orexin peptides act on two G protein-coupled receptors: orexin 1 receptor (OX1R) and orexin 2 receptor (OX2R). OX2R knockout (KO) mice, but n...