NTNT 185

Names

[ Name ]:
NTNT 185

Biological Activity

[Description]:

YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor)

Research Areas >> Neurological Disease

[Target]

OX2 Receptor:0.028 μM (EC50)

OX1 Receptor:2.75 μM (EC50)

[In Vivo]

YNT-185 dihydrochloride (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]. Animal Model: Male wild-type C57BL/6J mice[2] Dosage: 20, 40 mg/kg Administration: I.p. Result: Wake time was also significantly increased.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₃H₃₉Cl₂N₅O₅S

[ Molecular Weight ]:
688.66

NTNT 185

Names

Biological Activity

Chemical & Physical Properties

Related Compounds