narcolepsy

CRL-40940 is a selective dopaminergic reuptake inhibitor

OX2R agonist 1 is an OX2R activator with an EC50 of less than 100 nM. It is utilized in research related to narcolepsy and cataplexy.

Pitolisant is a potent and selective nonimidazole inverse agonist that targets the recombinant human histamine H3 receptor, with a Ki of 0.16 nM.

Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1) orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

Samelisant (SUVN-G3031) is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy.

YNT-185 is a nonpeptide, selective agonist of the orexin type-2 receptor (OX2R), with EC50 values of 0.028 μM for OX2R and 2.75 μM for OX1R. Additionally, YNT-185 effectively alleviates symptoms of narcolepsy-cataplexy in mouse models.

GSK 189254A is a histamine H3 receptor antagonist for the treatment of narcolepsy. Histamine H3 receptor antagonists have been shown to increase the release of neurotransmitters in the brain and to enhance cognition in vivo. The compound may also be usefu

Firazorexton hydrate (TAK-994) is a brain-penetrant, orally active agonist of the orexin type 2 receptor (OX2R) with a potent EC50 of 19 nM, effectively reducing wakefulness fragmentation and cataplexy-like episodes in mouse models of narcolepsy [1].

RTIOXA-43 is an OX2R OX1R (orexin receptor) dual agonist that increases wakefulness and attenuates episodic sleep symptoms and is commonly used in studies related to narcolepsy and neural signaling.

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

Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.