YNT 185 |
رقم الكتالوجGC50559 |
YNT 185 هو ناهض لمستقبلات الأوركسين من النوع 2 غير الببتيد الانتقائي (OX2R) ، مع EC50s من 0.028 و 2.75 μ ؛ M لـ OX2R و OX1R ، على التوالي.
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Cas No.: 1804978-82-2
Sample solution is provided at 25 µL, 10mM.
Potent and selective orexin OX2 receptor agonist (EC50 = 28 nM at human OX2 expressed in CHO cells). Displays approximately 100-fold selectivity for OX2 over OX1 (EC50 = 2.75 μM at human OX1 expressed in CHO cells). Depolarizes OX2-expressing histaminergic neurons in mouse brain slices. Increases wake time in wild type mice. Suppresses cataplexy-like symptoms in OX knockout mice.
Nagahara et al (2015) Design and synthesis of non-peptide, selective orexin receptor 2 agonists. J.Med.Chem. 58 7931 PMID:26267383 |Irukayama-Tomobe et al (2017) Nonpeptide orexin type-2 receptor agonist ameliorates narcolepsy-cataplexy symptoms in mouse models. Proc.Natl.Acad.Sci.USA. 144 5731 PMID:28507129
Average Rating: 5
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