0002 An Orexin 2 Receptor-selective Agonist, TAK-925, Shows Robust Wake-promoting Effects In Mice And Non-human Primates
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چکیده
منابع مشابه
Orexin receptor agonist Yan 7874 is a weak agonist of orexin/hypocretin receptors and shows orexin receptor-independent cytotoxicity
Two promising lead structures of small molecular orexin receptor agonist have been reported, but without detailed analyses of the pharmacological properties. One of them, 1-(3,4-dichlorophenyl)-2-[2-imino-3-(4-methylbenzyl)-2,3-dihydro-1H-benzo[d]imidazol-1-yl]ethan-1-ol (Yan 7874), is commercially available, and we set out to analyze its properties. As test system we utilized human OX1 and OX2...
متن کاملWake-promoting effects of orexin: Its independent actions against the background of an impaired corticotropine-releasing hormone receptor system.
It is widely accepted that orexin (hypocretin) bears wake-promoting effects. While under normal conditions the circadian rhythm of orexin release has a clear circadian distribution, the amplitude of orexin fluctuation is dampened in depression. Interestingly, clinical symptoms of depression include several sleep disturbances. In this disease, corticotropin-releasing hormone (CRH) seems to be an...
متن کاملCEP-26401 (irdabisant), a potent and selective histamine H₃ receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities.
CEP-26401 [irdabisant; 6-{4-[3-((R)-2-methyl-pyrrolidin-1-yl)-propoxy]-phenyl}-2H-pyridazin-3-one HCl] is a novel, potent histamine H₃ receptor (H₃R) antagonist/inverse agonist with drug-like properties. High affinity of CEP-26401 for H₃R was demonstrated in radioligand binding displacement assays in rat brain membranes (K(i) = 2.7 ± 0.3 nM) and recombinant rat and human H₃R-expressing systems ...
متن کاملCEP-26401 (Irdabisant), a Potent and Selective Histamine H3 Receptor Antagonist/Inverse Agonist with Cognition-Enhancing and Wake-Promoting Activities
CEP-26401 [irdabisant; 6-{4-[3-((R)-2-methyl-pyrrolidin-1-yl)propoxy]-phenyl}-2H-pyridazin-3-one HCl] is a novel, potent histamine H3 receptor (H3R) antagonist/inverse agonist with drug-like properties. High affinity of CEP-26401 for H3R was demonstrated in radioligand binding displacement assays in rat brain membranes (Ki 2.7 0.3 nM) and recombinant rat and human H3R-expressing systems (Ki 7.2...
متن کاملWake-promoting effects of vagus nerve stimulation after traumatic brain injury: upregulation of orexin-A and orexin receptor type 1 expression in the prefrontal cortex
Orexins, produced in the lateral hypothalamus, are important neuropeptides that participate in the sleep/wake cycle, and their expression coincides with the projection area of the vagus nerve in the brain. Vagus nerve stimulation has been shown to decrease the amounts of daytime sleep and rapid eye movement in epilepsy patients with traumatic brain injury. In the present study, we investigated ...
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ژورنال
عنوان ژورنال: Sleep
سال: 2018
ISSN: 0161-8105,1550-9109
DOI: 10.1093/sleep/zsy061.001