YNT-185 is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC 50 s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models [1] [2].
In Vivo, YNT-185 (20-40 mg/kg; i.p.) increases wakefulness in mice[2]. YNT-185 (300 nmol; i.c.v.) significantly increases wake time for 3 hours in a dose-dependent manner, accompanied by a decrease in NREM sleep time, in wild-type mice but not in OXRDKO mice[2].
References:
[1]. Nagahara T, et al. Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. J Med Chem. 2015;58(20):7931-7937.
[2]. Irukayama-Tomobe Y, et al. Nonpeptide orexin type-2 receptor agonist ameliorates narcolepsy-cataplexy symptoms in mouse models. Proc Natl Acad Sci U S A. 2017;114(22):5731-5736.
In Vivo, YNT-185 (20-40 mg/kg; i.p.) increases wakefulness in mice[2]. YNT-185 (300 nmol; i.c.v.) significantly increases wake time for 3 hours in a dose-dependent manner, accompanied by a decrease in NREM sleep time, in wild-type mice but not in OXRDKO mice[2].
References:
[1]. Nagahara T, et al. Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. J Med Chem. 2015;58(20):7931-7937.
[2]. Irukayama-Tomobe Y, et al. Nonpeptide orexin type-2 receptor agonist ameliorates narcolepsy-cataplexy symptoms in mouse models. Proc Natl Acad Sci U S A. 2017;114(22):5731-5736.