orexin (hypocretin) receptor
Formulation development for the orexin receptor antagonist almorexant: assessment in two clinical studies
... Abstract: Almorexant, a dual orexin receptor antagonist, was investigated for the treatment of insomnia. The following observations initiated further formulation development: the active pharmaceutical ...
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The orexin/receptor system : molecular mechanism and therapeutic potential for neurological diseases
... Although orexin-containing neurons are distributed only in the LH and adjacent areas, their nerve fibers project widely to multiple brain regions (Chen et ...Furthermore, orexin receptors exhibit a diffuse ...
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Signaling transduction regulated by 5 hydroxytryptamine 1A receptor and orexin receptor 2 heterodimers
... Analogously, orexin receptor 2 (OX2R) expresses extensively in adult brain including cerebral cortex, hippocampus and cerebellum ...ligand orexin A or orexin B stimulation ...that ...
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Dual agonist occupancy of orexin receptor 1 and cholecystokinin A receptor heterodimers decreases G protein dependent signaling and migration in the human colon cancer cell line HT 29
... κ-opioid receptor (KOR) affects cAMP accumulation after treatment with apelin-13 or DynA(1–13) ...of orexin receptor and corticotropin-releasing factor receptor serve as targets for cocaine ...
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Unilateral Hypothalamus Inactivation Prevents PTZ Kindling Development through Hippocampal Orexin Receptor 1 Modulation
... in, orexin-A and orexin-B, and orexin receptor is a mem- ber of GPCR family with two receptor subtypes; orexin receptor 1 (OX1R) and orexin receptor 2 ...
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Novel class of medications, orexin receptor antagonists, in the treatment of insomnia – critical appraisal of suvorexant
... nonbenzodiazepine receptor agonists, and melatonin agonists. Dual orexin receptor antagonists represent a new class of medications for the treatment of insomnia, which block the binding of ...
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Accelerated Development of the Dual Orexin Receptor Antagonist ACT-541468: Integration of a Microtracer in a First-in-Human Study
... Figure S1: Mean (±SD) concentration-time profile of total radioactivity in whole blood and plasma following oral administration of 50 mg ACT-541468 in combination with an oral microtrace[r] ...
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The role of orexin in post-stroke inflammation, cognitive decline, and depression
... to orexin receptor activation is increased intracellular Ca 2+ influx by pro- tein kinase C-dependent activation or voltage-gated Ca 2+ receptors ...activated orexin receptors involve the activity of ...
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Associations between the orexin (hypocretin) receptor 2 gene polymorphism Val308Ile and nicotine dependence in genome-wide and subsequent association studies
... encodes orexin receptor 2. The orexin receptor has two subtypes (orexin receptor 1 [HCRTR1] and orexin receptor 2 [HCRTR2]) and two known neuro- peptide ligands ...
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<p><em>Orexin/Hypocretin Type 2 Receptor</em> (<em>HCRTR2</em>) Gene as a Candidate Gene in Sertraline-Associated Insomnia in Depressed Patients</p>
... control. Orexin/hypocretin has been found in the hypothalamus areas rich in sleep-active ...that orexin and its receptors have a substantial role in conduct- ing the sleep/wakefulness ...of orexin ...
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Non-Destructive Determination of Magnetic Audio Tape Degradation for Various Tape Chemistries Using Spectroscopy and Chemometrics
... hypothalamic orexin (hypocretin) system, a central integrator of physiological function, plays an important role in modulating ...dual-orexin receptor antagonists are available for various clinical ...
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Suvorexant: a promising, novel treatment for insomnia
... first orexin receptor antagonist approved for the treatment of sleep onset and sleep maintenance insomnia holds promise for patients suffering from ...
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Antistress effects of Kampo medicine "Yokukansan" via regulation of orexin secretion
... plasma orexin levels compared with non-treated rats, whereas the administration of 1,000 mg/kg of YKS had no effect on orexin ...of orexin and corticosterone were ...and orexin significantly ...
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<p>Reduced plasma orexin-A levels in patients with bipolar disorder</p>
... recently, orexin has been studied extensively in patients with narcolepsy whose cerebrospinal fl uid (CSF) orexin levels were found to be very ...The orexin system plays a role not only in sleep awake ...
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The in vitro effect of progesterone on the orexin system in porcine uterine tissues during early pregnancy
... Background: Orexin A (OXA) and orexin B (OXB) are hypothalamic-derived peptides that participate in the regulation of energy metabolism, food intake and reproductive function by influencing the ...
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Systemic administration of orexin A ameliorates established experimental autoimmune encephalomyelitis by diminishing neuroinflammation
... delivered orexin A effects may modulate local (CNS) and/or peripheral immune ...found orexin receptor expression in both CNS and im- mune tissues of naïve ...hypothalamic orexin ...
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Original Article Orexin A stimulates Foxo1 phosphorylation via OX1R-induced PI3K/AKT and MAPK/ERK signaling pathways in hepatocytes
... Abstract: Orexin A and B are multifunctional neuropeptides implicated in the regulation of food intake, energy me- tabolism, glucose regulation, and ...(GPCR), orexin receptor 1 and orexin ...
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Profile of suvorexant in the management of insomnia
... Abstract: Suvorexant, approved in late 2014 in the United States and Japan for the treat- ment of insomnia characterized by difficulty achieving and/or maintaining sleep, is a dual orexin receptor ...
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Orexin neurons suppress narcolepsy via 2 distinct efferent pathways
... studies in mice. Thus, it is tempting to speculate a species differ- ence with respect to orexin receptor expression, for example, that OX2R is the predominant subtype in the DR serotonergic neu- rons of ...
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Original Article Vagus nerve stimulation causes wake-promotion by affecting neurotransmitters via orexins pathway in traumatic brain injury induced comatose rats
... an orexin receptor 1 antagonist, by intracerebroventricular injection and ...of orexin receptor-1 (OX1R), N Methyl D Aspartate receptor-1 (NMDAR1), 5-hydroxytryptamine 2A ...
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