Gene Symbol: HCRTR1
Description: hypocretin receptor 1
Alias: OX1R, orexin receptor type 1, hypocretin (orexin) receptor 1, hypocretin receptor type 1, orexin receptor 1, ox-1-R, ox1-R
Species: human
Products:     HCRTR1

Top Publications

  1. Sakurai T, Amemiya A, Ishii M, Matsuzaki I, Chemelli R, Tanaka H, et al. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell. 1998;92:573-85 pubmed
    ..prepro-orexin mRNA level is up-regulated upon fasting, suggesting a physiological role for the peptides as mediators in the central feedback mechanism that regulates feeding behavior. ..
  2. Holmqvist T, Johansson L, Ostman M, Ammoun S, Akerman K, Kukkonen J. OX1 orexin receptors couple to adenylyl cyclase regulation via multiple mechanisms. J Biol Chem. 2005;280:6570-9 pubmed
  3. Meerabux J, Iwayama Y, Sakurai T, Ohba H, Toyota T, Yamada K, et al. Association of an orexin 1 receptor 408Val variant with polydipsia-hyponatremia in schizophrenic subjects. Biol Psychiatry. 2005;58:401-7 pubmed
    ..I/D) sequence polymorphism of ACE and single nucleotide polymorphisms within the prepro-orexin (HCRT), orexin receptor 1 (HCRTR1), and orexin receptor 2 (HCRTR2) genes...
  4. de Lecea L, Kilduff T, Peyron C, Gao X, Foye P, Danielson P, et al. The hypocretins: hypothalamus-specific peptides with neuroexcitatory activity. Proc Natl Acad Sci U S A. 1998;95:322-7 pubmed
    ..One of the Hcrt peptides was excitatory when applied to cultured, synaptically coupled hypothalamic neurons, but not hippocampal neurons. These observations suggest that the hypocretins function within the CNS as neurotransmitters. ..
  5. Peyron C, Faraco J, Rogers W, Ripley B, Overeem S, Charnay Y, et al. A mutation in a case of early onset narcolepsy and a generalized absence of hypocretin peptides in human narcoleptic brains. Nat Med. 2000;6:991-7 pubmed
    ..of hypocretins in human narcolepsy through histopathology of six narcolepsy brains and mutation screening of Hcrt, Hcrtr1 and Hcrtr2 in 74 patients of various human leukocyte antigen and family history status...
  6. Voisin T, El Firar A, Rouyer Fessard C, Gratio V, Laburthe M. A hallmark of immunoreceptor, the tyrosine-based inhibitory motif ITIM, is present in the G protein-coupled receptor OX1R for orexins and drives apoptosis: a novel mechanism. FASEB J. 2008;22:1993-2002 pubmed publisher
    Orexins acting at the G protein-coupled receptor (GPCR) OX1R have recently been shown to promote dramatic apoptosis in cancer cells...
  7. El Firar A, Voisin T, Rouyer Fessard C, Ostuni M, Couvineau A, Laburthe M. Discovery of a functional immunoreceptor tyrosine-based switch motif in a 7-transmembrane-spanning receptor: role in the orexin receptor OX1R-driven apoptosis. FASEB J. 2009;23:4069-80 pubmed publisher
    ..We have recently shown that the 7-transmembrane-spanning orexin receptor OX1R mediates apoptosis through an original mechanism...
  8. Blais A, Drouin G, Chaumontet C, Voisin T, Couvelard A, Even P, et al. Impact of Orexin-A Treatment on Food Intake, Energy Metabolism and Body Weight in Mice. PLoS ONE. 2017;12:e0169908 pubmed publisher
    ..HCRT), and Y2 and Y5 neuropeptide Y, MC4 (melanocortin), OX1 and OX2 orexin receptors (Y2R, Y5R, MC4R, OX1R and OX2R, respectively) was also explored...
  9. Misawa K, Imai A, Mochizuki D, Misawa Y, Endo S, Hosokawa S, et al. Genes encoding neuropeptide receptors are epigenetic markers in patients with head and neck cancer: a site-specific analysis. Oncotarget. 2017;8:76318-76328 pubmed publisher
    ..The NPFFR1, NPFFR2, HCRTR1, HCRTR2, NPY1R, NPY2R, NPY4R, and NPY5R promoters were methylated in 80...

More Information

Publications119 found, 100 shown here

  1. Zhang X, Zhu J, Geng W, Zhao S, Jiang C, Cai S, et al. Electroacupuncture at Feishu (BL13) and Zusanli (ST36) down-regulates the expression of orexins and their receptors in rats with chronic obstructive pulmonary disease. J Integr Med. 2014;12:417-24 pubmed publisher
    ..Orexin A, but not orexinB, levels in lung tissue also decreased (P<0.01), as did mRNA expression of OX1R and OX2R in lung tissue (P<0.05 and P<0.01, respectively)...
  2. Gonzalez B, Torres O, Jayanthi S, Gomez N, Sosa M, Bernardi A, et al. The effects of single-dose injections of modafinil and methamphetamine on epigenetic and functional markers in the mouse medial prefrontal cortex: potential role of dopamine receptors. Prog Neuropsychopharmacol Biol Psychiatry. 2019;88:222-234 pubmed publisher
    ..Hrh1, but METH increasing H4ac at Drd1; iii) comparable effects of both psychostimulants, increasing H3ac at Drd2, Hcrtr1, and Hrh1 promoters, decreasing H3ac at Hrh3, increasing H4ac at Hcrtr1, and decreasing H4ac at Hcrtr2, Hrh3, and ..
  3. Tarasiuk A, Levi A, Assadi M, Troib A, Segev Y. Orexin Plays a Role in Growth Impediment Induced by Obstructive Sleep Breathing in Rats. Sleep. 2016;39:887-97 pubmed publisher
    ..The impediment of bone elongation and bone mass was followed by a 200% increase in OX1R and 38% reduction of local GP ghrelin proteins and growth hormone secretagogue receptor 1a...
  4. Singh A, Zhao K. Treatment of Insomnia With Traditional Chinese Herbal Medicine. Int Rev Neurobiol. 2017;135:97-115 pubmed publisher
  5. Sato K, Tsuji A, Usumoto Y, Kudo K, Yokoyama T, Ikeda N. Expression of mRNA in the frontal cortex and hypothalamus in a rat model of acute carbon dioxide poisoning. Leg Med (Tokyo). 2016;19:101-6 pubmed publisher
    ..Ppy), corticotropin releasing hormone receptor 2 (Crhr2), carbonic anhydrase 1 (Car1), and hypocretin receptor 1 (Hcrtr1) expressed in the hypothalamus...
  6. Wang D, Opperhuizen A, Reznick J, Turner N, Su Y, Cooney G, et al. Effects of feeding time on daily rhythms of neuropeptide and clock gene expression in the rat hypothalamus. Brain Res. 2017;1671:93-101 pubmed publisher
    ..In conclusion, feeding at the 'wrong' time-of-day not only induces desynchronization between brain and body clocks but also within the hypothalamus, which may contribute further to the underlying pathology of metabolic dysregulation. ..
  7. Kowalska M, Prendecki M, Kozubski W, Lianeri M, Dorszewska J. Molecular factors in migraine. Oncotarget. 2016;7:50708-50718 pubmed publisher
    ..The genes analysed in familial and sporadic migraine are: MTHFR, KCNK18, HCRTR1, SLC6A4, STX1A, GRIA1 and GRIA3. It is possible that migraine is a multifactorial disease with polygenic influence...
  8. Kaushik M, Aritake K, Imanishi A, Kanbayashi T, Ichikawa T, Shimizu T, et al. Continuous intrathecal orexin delivery inhibits cataplexy in a murine model of narcolepsy. Proc Natl Acad Sci U S A. 2018;115:6046-6051 pubmed publisher
    ..This study supports the concept of intrathecal orexin delivery as a potential therapy for narcolepsy-cataplexy to improve the well-being of patients. ..
  9. Kitajima S, Iwata Y, Furuichi K, Sagara A, Shinozaki Y, Toyama T, et al. Messenger RNA expression profile of sleep-related genes in peripheral blood cells in patients with chronic kidney disease. Clin Exp Nephrol. 2016;20:218-25 pubmed publisher
    ..Moreover, the mRNA expression of orexin and its receptor (HCRTR1 and HCRTR2) was also inversely correlated with renal function...
  10. Zhang L, Yang C, Ouyang P, Zhang Z, Ran M, Tong L, et al. Orexin-A facilitates emergence of the rat from isoflurane anesthesia via mediation of the basal forebrain. Neuropeptides. 2016;58:7-14 pubmed publisher
    ..The results indicate that orexin-A plays a promotive role in the emergence of isoflurane anesthesia and this effect is mediated by the basal forebrain. ..
  11. Olney J, Navarro M, Thiele T. The Role of Orexin Signaling in the Ventral Tegmental Area and Central Amygdala in Modulating Binge-Like Ethanol Drinking Behavior. Alcohol Clin Exp Res. 2017;41:551-561 pubmed publisher
    ..However, data from site-directed pharmacology studies indicate that the orexin-1 receptor (OX1R) is the predominate receptor subtype within the VTA and CeA that regulates binge-like EtOH drinking...
  12. Kaewsutthi S, Santiprabhob J, Phonrat B, Tungtrongchitr A, Lertrit P, Tungtrongchitr R. Exome sequencing in Thai patients with familial obesity. Genet Mol Res. 2016;15: pubmed publisher
    ..The minor allele frequency of 14 of these genes (ALOX5AP, COL9A2, DEFB126, GDPD4, HCRTR1, MLL3, OPLAH, OR4C45, PRIM2, RXFP2, TIGD6, TRPM8, USP49, and ZNF596) was low, indicating causal variants that ..
  13. Baccari M. Orexins and gastrointestinal functions. Curr Protein Pept Sci. 2010;11:148-55 pubmed
    ..orexin receptors have been shown to be widely distributed: both OXA and OXB act through two subtypes of receptors (OX1R and OX2R) that belong to the G protein-coupled superfamily of receptors...
  14. Davoudi M, Azizi H, Mirnajafi Zadeh J, Semnanian S. Decrease of inhibitory synaptic currents of locus coeruleus neurons via orexin type 1 receptors in the context of naloxone-induced morphine withdrawal. J Physiol Sci. 2019;69:281-293 pubmed publisher
    ..naloxone on eIPSCs amplitude and sIPSCs frequency but had no effect on the presence of the orexin type 1 receptor (OX1R) antagonist, SB-334867. Orexin-A alone had no significant effect on eIPSCs and sIPSCs in the absence of naloxone...
  15. Farzinpour Z, Taslimi Z, Azizbeigi R, Karimi Haghighi S, Haghparast A. Involvement of orexinergic receptors in the nucleus accumbens, in the effect of forced swim stress on the reinstatement of morphine seeking behaviors. Behav Brain Res. 2019;356:279-287 pubmed publisher
    ..The extinguished rats received intra-NAc injection of SB334867 as OX1R antagonist or TCSOX229 as OX2R antagonist before effective priming dose injection of morphine (1 mg/kg; sc)...
  16. Gotter A, Forman M, Harrell C, Stevens J, Svetnik V, Yee K, et al. Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man. Sci Rep. 2016;6:27147 pubmed publisher
    Orexin neuropeptides regulate sleep/wake through orexin receptors (OX1R, OX2R); OX2R is the predominant mediator of arousal promotion...
  17. Dimatelis J, Mtintsilana A, Naidoo V, Stein D, Russell V. Chronic light exposure alters serotonergic and orexinergic systems in the rat brain and reverses maternal separation-induced increase in orexin receptors in the prefrontal cortex. Metab Brain Dis. 2018;33:433-441 pubmed publisher
    ..Western blotting was used to measure orexin receptor 1 (OXR-1) and 2 (OXR-2) in the PFC. MS did not affect 5-HT levels in these rats...
  18. Cristino L, Luongo L, Imperatore R, Boccella S, Becker T, Morello G, et al. Orexin-A and Endocannabinoid Activation of the Descending Antinociceptive Pathway Underlies Altered Pain Perception in Leptin Signaling Deficiency. Neuropsychopharmacology. 2016;41:508-20 pubmed publisher
    ..We propose that OX-A/endocannabinoid cross talk in the descending antinociceptive pathway might partly underlie increased pain thresholds in conditions associated with impaired leptin signaling. ..
  19. Goudarzi E, Elahdadi Salmani M, Lashkarbolouki T, Goudarzi I. Hippocampal orexin receptors inactivation reduces PTZ induced seizures of male rats. Pharmacol Biochem Behav. 2015;130:77-83 pubmed publisher
    ..Orexin 1 receptor (OX1R) antagonist (SB) and OX2R antagonist (TCS) were administrated bilaterally through separate cannulae into both ..
  20. Wang Z, Liu S, Kakizaki M, Hirose Y, Ishikawa Y, Funato H, et al. Orexin/hypocretin activates mTOR complex 1 (mTORC1) via an Erk/Akt-independent and calcium-stimulated lysosome v-ATPase pathway. J Biol Chem. 2014;289:31950-9 pubmed publisher
    ..brain and multiple recombinant cell lines that express the G protein-coupled receptors (GPCRs), orexin 1 receptor (OX1R) or orexin 2 receptor (OX2R)...
  21. Deats S, Adidharma W, Yan L. Hypothalamic dopaminergic neurons in an animal model of seasonal affective disorder. Neurosci Lett. 2015;602:17-21 pubmed publisher
    ..We also found that treating BLD animals with a selective orexin receptor 1 (OX1R) antagonist SB-334867 significantly reduced the number of hypothalamic TH-ir cells...
  22. Ciuculete D, Boström A, Voisin S, Philipps H, Titova O, Bandstein M, et al. A methylome-wide mQTL analysis reveals associations of methylation sites with GAD1 and HDAC3 SNPs and a general psychiatric risk score. Transl Psychiatry. 2017;7:e1002 pubmed publisher
    ..We detected five SNPs (in HCRTR1, GAD1, HADC3 and FKBP5) that were associated with eight CpG sites, validating five of these SNP-CpG pairs...
  23. Van de Bittner G, Van de Bittner K, Wey H, Rowe W, Dharanipragada R, Ying X, et al. Positron Emission Tomography Assessment of the Intranasal Delivery Route for Orexin A. ACS Chem Neurosci. 2018;9:358-368 pubmed publisher
    ..intranasal delivery of Orexin A, a native neuropeptide and prospective antinarcoleptic drug that binds the orexin receptor 1. Using physicochemical and pharmacological analysis, we identified the methylation sites and confirmed the ..
  24. Ji M, Zhang X, Chen Z, Wang J, Zhu J. Orexin prevents depressive-like behavior by promoting stress resilience. Mol Psychiatry. 2019;24:282-293 pubmed publisher
    ..Two orexin receptors, OX1R and OX2R, and their downstream Na+-Ca2+ exchanger and L-type Ca2+ channel co-..
  25. Cole S, Mayer H, Petrovich G. Orexin/Hypocretin-1 Receptor Antagonism Selectively Reduces Cue-Induced Feeding in Sated Rats and Recruits Medial Prefrontal Cortex and Thalamus. Sci Rep. 2015;5:16143 pubmed publisher
    ..Systemic administration of the orexin-1 receptor (OX1R) antagonist SB-334867 had no effect on baseline eating, but significantly reduced cue-driven consumption in sated ..
  26. Lei K, Wegner S, Yu J, Hopf F. Orexin-1 receptor blockade suppresses compulsive-like alcohol drinking in mice. Neuropharmacology. 2016;110:431-437 pubmed publisher
    ..We found that systemic administration of the widely used selective orexin-1 receptor (OX1R) blocker, SB-334867 (SB), significantly reduced compulsive-like consumption at doses lower than those reported to ..
  27. Martins L, Seoane Collazo P, CONTRERAS C, González García I, Martínez Sánchez N, González F, et al. A Functional Link between AMPK and Orexin Mediates the Effect of BMP8B on Energy Balance. Cell Rep. 2016;16:2231-2242 pubmed publisher
    ..is mediated by the inhibition of AMPK in the VMH and the subsequent increase in OX signaling via the OX receptor 1 (OX1R). Accordingly, the thermogenic effect of BMP8B is totally absent in ox-null mice...
  28. Huber M, Chen Q, Shan Z. The Orexin System and Hypertension. Cell Mol Neurobiol. 2018;38:385-391 pubmed publisher
    ..Furthermore, upregulation of the orexin receptor 1 increases firing of hypothalamic paraventricular nucleus neurons, augments SNA, and contributes to ..
  29. Khanday M, Mallick B. REM sleep modulation by perifornical orexinergic inputs to the pedunculo-pontine tegmental neurons in rats. Neuroscience. 2015;308:125-33 pubmed publisher
    ..by glutamate and simultaneously bilateral PPT neurons were infused with either saline or orexin receptor1 (OX1R) antagonist...
  30. Howland R. Suvorexant: a novel therapy for the treatment of insomnia. J Psychosoc Nurs Ment Health Serv. 2014;52:23-6 pubmed publisher
    Suvorexant is a pharmacologically novel dual antagonist of orexin receptors OX1R and OX2R, which has an effect that promotes sleep by reducing arousal and wakefulness...
  31. Lyons D, Hellysaz A, Ammari R, Broberger C. Hypocretin/Orexin Peptides Excite Rat Neuroendocrine Dopamine Neurons through Orexin 2 Receptor-Mediated Activation of a Mixed Cation Current. Sci Rep. 2017;7:41535 pubmed publisher
    ..consequence of OX2R receptor activation (as it was blocked by the OX2R receptor antagonist TCS OX2 29, but not the OX1R receptor antagonist SB 334867)...
  32. Riahi E, Arezoomandan R, Fatahi Z, Haghparast A. The electrical activity of hippocampal pyramidal neuron is subjected to descending control by the brain orexin/hypocretin system. Neurobiol Learn Mem. 2015;119:93-101 pubmed publisher
    ..c.v. injection of orexin-A 0.5 nmol, SB334867 400 nmol, a selective orexin receptor 1 antagonist, saline, or DMSO, or microinjection of carbachol 250 nmol or saline into the ipsilateral lateral ..
  33. Kordi Jaz E, Moghimi A, Fereidoni M, Asadi S, Shamsizadeh A, Roohbakhsh A. SB-334867, an orexin receptor 1 antagonist, decreased seizure and anxiety in pentylenetetrazol-kindled rats. Fundam Clin Pharmacol. 2017;31:201-207 pubmed publisher
    ..Based on the presented results, it is suggested that pharmacological blockade of the OX1 receptor is a potential target in the treatment of seizure and concomitant anxiety disorders. ..
  34. Spinazzi R, Rucinski M, Neri G, Malendowicz L, Nussdorfer G. Preproorexin and orexin receptors are expressed in cortisol-secreting adrenocortical adenomas, and orexins stimulate in vitro cortisol secretion and growth of tumor cells. J Clin Endocrinol Metab. 2005;90:3544-9 pubmed
  35. Putula J, Pihlajamaa T, Kukkonen J. Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery. Br J Pharmacol. 2014;171:5816-28 pubmed publisher
    ..From a drug discovery perspective, further experiments need to identify the target for Ca(2+) in orexin-A-OX1 receptor interaction and its mechanism of action. ..
  36. Robinson J, McDonald P. The orexin 1 receptor modulates kappa opioid receptor function via a JNK-dependent mechanism. Cell Signal. 2015;27:1449-56 pubmed publisher
    The orexin 1 receptor (OX1R) and the kappa opioid receptor (KOR) are two G protein-coupled receptors (GPCRs) previously demonstrated to play important roles in modulating the rewarding effects of drugs of abuse such as cocaine...
  37. Sadeghzadeh F, Namvar P, Naghavi F, Haghparast A. Differential effects of intra-accumbal orexin-1 and -2 receptor antagonists on the expression and extinction of morphine-induced conditioned place preference in rats. Pharmacol Biochem Behav. 2016;142:8-14 pubmed publisher
    ..an attempt was made to determine the effects of intra-accumbal administration of SB334867 as an orexin-1 receptor (OX1R) antagonist and TCS OX2 29 as an orexin-2 receptor (OX2R) antagonist in the expression and maintenance of morphine-..
  38. Shu Q, Zhang J, Ma W, Lei Y, Zhou D. Orexin-A promotes Glu uptake by OX1R/PKC?/ERK1/2/GLT-1 pathway in astrocytes and protects co-cultured astrocytes and neurons against apoptosis in anoxia/hypoglycemic injury in vitro. Mol Cell Biochem. 2017;425:103-112 pubmed publisher
    ..However, these effects were significantly weakened by treatment with orexin-A receptor 1 (OX1R) antagonist...
  39. Willie J, Chemelli R, Sinton C, Yanagisawa M. To eat or to sleep? Orexin in the regulation of feeding and wakefulness. Annu Rev Neurosci. 2001;24:429-58 pubmed
  40. Ibrahim B, Abdel Rahman A. A pivotal role for enhanced brainstem Orexin receptor 1 signaling in the central cannabinoid receptor 1-mediated pressor response in conscious rats. Brain Res. 2015;1622:51-63 pubmed publisher
    b>Orexin receptor 1 (OX1R) signaling is implicated in cannabinoid receptor 1 (CB1R) modulation of feeding...
  41. Peng X, Guo F, Sun X, Gong Y, Xu L. [Effect of orexin-A and orexin-1 receptor antagonist injected into the fourth ventricle of rats on food-intake and spontaneous physical activity]. Sheng Li Xue Bao. 2015;67:379-85 pubmed
    The present study was aimed to investigate the effects of orexin-A and orexin-1 receptor (OX1R) antagonist injected into the fourth ventricle of rats on food-intake and spontaneous physical activity (SPA)...
  42. Han F. Respiratory regulation in narcolepsy. Sleep Breath. 2012;16:241-5 pubmed publisher
    ..Unlike in mouse, hypocretin-1 is not a major factor contributing to chemoresponsiveness in human. Species differences may exist. ..
  43. Liu F, Weng S, Yang X, Zhong Y. Orexin-A potentiates L-type calcium/barium currents in rat retinal ganglion cells. Neuroscience. 2015;305:225-37 pubmed publisher
    ..behaviors via the activation of two subtypes of G-protein-coupled receptors: orexin 1 and orexin 2 receptors (OX1R and OX2R)...
  44. Fatemi I, Shamsizadeh A, Roohbakhsh A, Ayoobi F, Sanati M, Motevalian M. Increase in mRNA Level of Orexin1 and 2 Receptors Following Induction of Experimental Autoimmune Encephalomyelitis in Mice. Iran J Allergy Asthma Immunol. 2016;15:20-6 pubmed
    ..Then, the expression profiles of prepro-orexin, orexin 1 receptors (OX1R) and orexin 2 receptors (OX2R) in hypothalamic region were assessed using real-time PCR method...
  45. Kooshki R, Abbasnejad M, Esmaeili Mahani S, Raoof M. The role of trigeminal nucleus caudalis orexin 1 receptors in orofacial pain transmission and in orofacial pain-induced learning and memory impairment in rats. Physiol Behav. 2016;157:20-7 pubmed publisher
    ..Orexin 1 receptor (OX1R) has been reported in trigeminal nucleus caudalis...
  46. Abbas M, Shoji H, Soya S, Hondo M, Miyakawa T, Sakurai T. Comprehensive Behavioral Analysis of Male Ox1r (-/-) Mice Showed Implication of Orexin Receptor-1 in Mood, Anxiety, and Social Behavior. Front Behav Neurosci. 2015;9:324 pubmed publisher
    ..Recent pharmacological studies using selective antagonists have suggested that orexin receptor-1 (OX1R) is involved in physiological processes that regulate emotion, the reward system, and autonomic nervous system...
  47. Czerwińska J, Chojnowska K, Kaminski T, Bogacka I, Smolinska N, Kaminska B. Orexin receptor expression in the hypothalamic-pituitary-adrenal and hypothalamic-pituitary-gonadal axes of free-living European beavers (Castor fiber L.) in different periods of the reproductive cycle. Gen Comp Endocrinol. 2017;240:103-113 pubmed publisher
    Orexins are hypothalamic neuropeptides acting via two G protein-coupled receptors in mammals: orexin receptor 1 (OX1R) and orexin receptor 2 (OX2R)...
  48. Joshi D, Singh S. Localization and expression of Orexin A and its receptor in mouse testis during different stages of postnatal development. Gen Comp Endocrinol. 2017;241:50-56 pubmed publisher
    ..in regulation of various biological functions and its actions are mediated through G-protein-coupled receptor, OX1R. This neuropeptide has emerged as a central neuroendocrine modulator of reproductive functions...
  49. Pruszynska Oszmalek E, Kolodziejski P, Kaczmarek P, Sassek M, Szczepankiewicz D, Mikula R, et al. Orexin A but not orexin B regulates lipid metabolism and leptin secretion in isolated porcine adipocytes. Domest Anim Endocrinol. 2018;63:59-68 pubmed publisher
    ..According to the results, both orexin receptor 1 and orexin receptor 2 were expressed in the porcine adipose tissue...
  50. Blanco M, Lopez M, Garcia Caballero T, Gallego R, Vázquez Boquete A -, Morel G, et al. Cellular localization of orexin receptors in human pituitary. J Clin Endocrinol Metab. 2001;86:1616-9 pubmed
    ..They act on G protein receptors named orexin receptor 1 (OX(1)R) and orexin receptor 2 (OX(2)R), respectively...
  51. Farahimanesh S, Karimi S, Haghparast A. Role of orexin-1 receptors in the dorsal hippocampus (CA1 region) in expression and extinction of the morphine-induced conditioned place preference in the rats. Peptides. 2018;101:25-31 pubmed publisher
    ..Objectives here, we investigated the effect of intra-hippocampal CA1 administration of orexin-1 receptor (OX1r) antagonist on the expression, and extinction of morphine-induced place preference in rats...
  52. Rainero I, Ostacoli L, Rubino E, Gallone S, Picci L, Fenoglio P, et al. Association between major mood disorders and the hypocretin receptor 1 gene. J Affect Disord. 2011;130:487-91 pubmed publisher
    ..involvement in MMD evaluating whether particular alleles or genotypes of the hypocretin pathway genes (HCRT, HCRTR1 and HCRTR2) would modify the occurrence and clinical features of the disease...
  53. Fukunaka Y, Shinkai T, Hwang R, Hori H, Utsunomiya K, Sakata S, et al. The orexin 1 receptor (HCRTR1) gene as a susceptibility gene contributing to polydipsia-hyponatremia in schizophrenia. Neuromolecular Med. 2007;9:292-7 pubmed
    ..2005 Biol Psychiatry 58 401-407] reported an association between the 408Val allele of the orexin 1 receptor (HCRTR1) gene and polydipsia-hyponatremia in a sample of Japanese patients with SCZ...
  54. Xu T, Ward R, Pediani J, Milligan G. Intramolecular fluorescence resonance energy transfer (FRET) sensors of the orexin OX1 and OX2 receptors identify slow kinetics of agonist activation. J Biol Chem. 2012;287:14937-49 pubmed publisher
    ..Such sensors provide means to assess the kinetics of receptor activation and how this may be altered by mutation and sequence variation of the receptors. ..
  55. Johnson P, Federici L, Fitz S, Renger J, Shireman B, Winrow C, et al. OREXIN 1 AND 2 RECEPTOR INVOLVEMENT IN CO2 -INDUCED PANIC-ASSOCIATED BEHAVIOR AND AUTONOMIC RESPONSES. Depress Anxiety. 2015;32:671-83 pubmed publisher
    ..2 receptor (OX2R) most robustly maps to the histaminergic wake-promoting region, while the orexin 1 receptor (OX1R) distribution is more exclusive and dense in anxiety and panic circuitry regions, such as the locus ceruleus...
  56. Esmaeili M, Reisi Z, Ezzatpanah S, Haghparast A. Role of orexin-2 and CB1 receptors within the periaqueductal gray matter in lateral hypothalamic-induced antinociception in rats. Behav Pharmacol. 2017;28:83-89 pubmed publisher
    Orexin plays an important role in pain modulation. Orexin-1 and orexin-2 receptors (Ox1r and Ox2r) are found at high density in the ventrolateral periaqueductal gray matter (vlPAG)...
  57. Duguay D, Bélanger Nelson E, Mongrain V, Beben A, Khatchadourian A, Cermakian N. Dynein light chain Tctex-type 1 modulates orexin signaling through its interaction with orexin 1 receptor. PLoS ONE. 2011;6:e26430 pubmed publisher
    ..involved in the regulation of the sleep-wake cycle, feeding and reward, via activation of orexin receptors 1 and 2 (OX1R, OX2R). The loss of orexin peptides or functional OX2R has been shown to cause the sleep disorder, narcolepsy...
  58. Kukkonen J. G-protein-dependency of orexin/hypocretin receptor signalling in recombinant Chinese hamster ovary cells. Biochem Biophys Res Commun. 2016;476:379-385 pubmed publisher
    ..AC regulation warrants more studies. ..
  59. Bahaaddini M, Khatamsaz S, Esmaeili Mahani S, Abbasnejad M, Raoof M. The role of trigeminal nucleus caudalis orexin 1 receptor in orofacial pain-induced anxiety in rat. Neuroreport. 2016;27:1107-13 pubmed publisher
    ..This study was designed to evaluate the role of orexin 1 receptors (OX1R) within trigeminal nucleus caudalis (TNC) in anxiety following the induction of orofacial pain...
  60. Bai B, Chen X, Zhang R, Wang X, Jiang Y, Li D, et al. 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. Biochim Biophys Acta Mol Cell Res. 2017;1864:1153-1164 pubmed publisher
    The orexin (OX1R) and cholecystokinin A (CCK1R) receptors play opposing roles in the migration of the human colon cancer cell line HT-29, and may be involved in the pathogenesis and pathophysiology of cancer cell invasion and metastasis...
  61. Olafsdóttir B, Rye D, Scammell T, Matheson J, Stefansson K, Gulcher J. Polymorphisms in hypocretin/orexin pathway genes and narcolepsy. Neurology. 2001;57:1896-9 pubmed
  62. Benarroch E, Schmeichel A, Sandroni P, Low P, Parisi J. Involvement of hypocretin neurons in multiple system atrophy. Acta Neuropathol. 2007;113:75-80 pubmed
    ..This is the first demonstration of loss of Hcrt/Orx neurons in MSA, which is consistent with a system degeneration of neurons involved in homeostatic function, including sleep and autonomic regulation, in this disorder. ..
  63. Mavanji V, Butterick T, Duffy C, Nixon J, Billington C, Kotz C. Orexin/hypocretin treatment restores hippocampal-dependent memory in orexin-deficient mice. Neurobiol Learn Mem. 2017;146:21-30 pubmed publisher
    ..We first measured hippocampal orexin receptor 1 (OX1R) gene expression and protein levels, then tested acquisition and consolidation of two-way active ..
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    ..I seek to provide a comprehensive update of orexin physiology that spans from the molecular players in orexin receptor signaling to the systemic responses yet emphasizing the cellular physiological aspects of this system. ..
  66. Soya S, Takahashi T, McHugh T, Maejima T, Herlitze S, Abe M, et al. Orexin modulates behavioral fear expression through the locus coeruleus. Nat Commun. 2017;8:1606 pubmed publisher
    ..Pharmacogenetic/optogenetic silencing of this circuit as well as acute blockade of the orexin receptor-1 (OX1R) decreases conditioned fear responses...
  67. Yin J, Babaoglu K, Brautigam C, Clark L, Shao Z, Scheuermann T, et al. Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors. Nat Struct Mol Biol. 2016;23:293-9 pubmed publisher
    ..We determined structures of hOX1R bound to the OX1R-selective antagonist SB-674042 and the dual antagonist suvorexant at 2.8-Ã… and 2...
  68. Rouault A, Lee A, Sebag J. Regions of MRAP2 required for the inhibition of orexin and prokineticin receptor signaling. Biochim Biophys Acta Mol Cell Res. 2017;1864:2322-2329 pubmed publisher
    ..In this study we demonstrate a new role of MRAP2 in the regulation of the orexin receptor 1 (OX1R) and identify the specific regions of MRAP2 required for the regulation of OX1R and PKR1...
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    ..The response coincided with other high-potency lipid messenger responses, and may interact with these signals. ..
  71. Huber M, Fan Y, Jiang E, Zhu F, Larson R, Yan J, et al. Increased activity of the orexin system in the paraventricular nucleus contributes to salt-sensitive hypertension. Am J Physiol Heart Circ Physiol. 2017;313:H1075-H1086 pubmed publisher
    ..4% NaCl) diet for 4 wk. HS intake did not alter mean arterial pressure (MAP), PVN mRNA levels of orexin receptor 1 (OX1R), or OX2R but slightly increased PVN AVP mRNA expression in SD rats...
  72. Fakhari M, Azizi H, Semnanian S. Central antagonism of orexin type-1 receptors attenuates the development of morphine dependence in rat locus coeruleus neurons. Neuroscience. 2017;363:1-10 pubmed publisher
    ..In this study the effect of central OX1R blockade on neuronal activity and cAMP content of LC neurons was investigated following naloxone administration in ..
  73. Bernstein D, Badve P, Barson J, Bass C, Espana R. Hypocretin receptor 1 knockdown in the ventral tegmental area attenuates mesolimbic dopamine signaling and reduces motivation for cocaine. Addict Biol. 2018;23:1032-1045 pubmed publisher
    The hypocretin receptor 1 (HCRTr1) is a critical participant in the regulation of motivated behavior...
  74. Chang X, Zhao Y, Ju S, Guo L. Orexin-A regulates cell apoptosis in human H295R adrenocortical cells via orexin receptor type 1 through the AKT signaling pathway. Mol Med Rep. 2015;12:7582-8 pubmed publisher
    ..study, human H295R adrenocortical cells were exposed to orexin‑A (10‑10-10‑6 M), with orexin receptor type 1 (OX1 receptor) antagonist SB334867 or AKT antagonist PF‑04691502...
  75. Haghparast A, Shafiei I, Alizadeh A, Ezzatpanah S, Haghparast A. Blockade of the orexin receptors in the CA1 region of hippocampus decreased the lateral hypothalamic-induced antinociceptive responses in the model of orofacial formalin test in the rats. Peptides. 2018;99:217-222 pubmed publisher
    ..Intra-LH microinjection of carbachol was done 5min after intra-CA1 administration of SB-334867 (OX1R antagonist) or TCS OX2 29 (OX2R antagonist)...
  76. Peltonen H, Akerman K, Bart G. A role for PKD1 and PKD3 activation in modulation of calcium oscillations induced by orexin receptor 1 stimulation. Biochim Biophys Acta. 2010;1803:1206-12 pubmed publisher
    ..play an important role in the control of energy metabolism via either of two G-protein-coupled receptors, orexin receptor 1 (Ox1R) and 2...
  77. Xie X. The neuronal circuit between nociceptin/orphanin FQ and hypocretins/orexins coordinately modulates stress-induced analgesia and anxiety-related behavior. Vitam Horm. 2015;97:295-321 pubmed publisher
    ..The information obtained from these studies has provided insights into how interaction between the Hcrt and N/OFQ systems positively and negatively modulates the complex and integrated stress responses. ..
  78. Karhu L, Turku A, Xhaard H. Modeling of the OX1R-orexin-A complex suggests two alternative binding modes. BMC Struct Biol. 2015;15:9 pubmed publisher
    ..The binding modes should serve small molecule discovery, and offer insights into the mechanism of receptor activation. ..
  79. Futamura A, Nozawa D, Araki Y, Tamura Y, Tokura S, Kawamoto H, et al. Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide. Bioorg Med Chem. 2017;25:5203-5215 pubmed publisher
    The design, synthesis, and structure activity relationships of the novel class of pyrazolylethylbenzamide orexin receptor 1-selective antagonists are described...
  80. Mishima K, Fujiki N, Yoshida Y, Sakurai T, Honda M, Mignot E, et al. Hypocretin receptor expression in canine and murine narcolepsy models and in hypocretin-ligand deficient human narcolepsy. Sleep. 2008;31:1119-26 pubmed
    To determine whether hypocretin receptor gene (hcrtR1 and hcrtR2) expression is affected after long-term hypocretin ligand loss in humans and animal models of narcolepsy. Animal and human study...
  81. Peltonen H, Magga J, Bart G, Turunen P, Antikainen M, Kukkonen J, et al. Involvement of TRPC3 channels in calcium oscillations mediated by OX(1) orexin receptors. Biochem Biophys Res Commun. 2009;385:408-12 pubmed publisher
    ..However, as shown here in HEK293 cells 1 nM orexin-A (Ox-A) acting at OX1 receptors (OX1R) triggered oscillatory Ca2+ responses, requiring external Ca2+...
  82. Turunen P, Jäntti M, Kukkonen J. OX1 orexin/hypocretin receptor signaling through arachidonic acid and endocannabinoid release. Mol Pharmacol. 2012;82:156-67 pubmed publisher
    ..g., in neurons). ..
  83. Huang Y, Guilleminault C, Chen C, Lai P, Hwang F. Narcolepsy-cataplexy and schizophrenia in adolescents. Sleep Med. 2014;15:15-22 pubmed publisher
    ..difference in HLA-DR typing, tumor necrosis factor ? (TNF-?) levels, hypocretin (orexin) receptor 1 gene, HCRTR1, and the hypocretin (orexin) receptor 2 gene, HCRTR2, or blood infectious titers...
  84. Chen J, Zhang R, Chen X, Wang C, Cai X, Liu H, et al. Heterodimerization of human orexin receptor 1 and kappa opioid receptor promotes protein kinase A/cAMP-response element binding protein signaling via a Gαs-mediated mechanism. Cell Signal. 2015;27:1426-38 pubmed publisher
    ..brain stimulation reward, and impulsivity in ventral tegmental area (VTA), where dopamine neurons express both OX1R and KORs...
  85. Ammoun S, Lindholm D, Wootz H, Akerman K, Kukkonen J. G-protein-coupled OX1 orexin/hcrtr-1 hypocretin receptors induce caspase-dependent and -independent cell death through p38 mitogen-/stress-activated protein kinase. J Biol Chem. 2006;281:834-42 pubmed
  86. Alexandre D, Hautot C, Mehio M, Jeandel L, Courel M, Voisin T, et al. The orexin type 1 receptor is overexpressed in advanced prostate cancer with a neuroendocrine differentiation, and mediates apoptosis. Eur J Cancer. 2014;50:2126-33 pubmed publisher
    ..We have localised the orexin type 1 and 2 receptors (OX1R and OX2R) and orexin A (OxA) in CaP sections of various grades and we have quantified tumour cells containing OX1R...
  87. Putula J, Turunen P, Johansson L, Näsman J, Ra R, Korhonen L, et al. Orexin/hypocretin receptor chimaeras reveal structural features important for orexin peptide distinction. FEBS Lett. 2011;585:1368-74 pubmed publisher
  88. Hilairet S, Bouaboula M, Carrière D, Le Fur G, Casellas P. Hypersensitization of the Orexin 1 receptor by the CB1 receptor: evidence for cross-talk blocked by the specific CB1 antagonist, SR141716. J Biol Chem. 2003;278:23731-7 pubmed
    ..present study, we observed evidence of cross-talk between the cannabinoid receptor CB1 and the orexin 1 receptor (OX1R) using a heterologous system...
  89. Ziolkowska A, Spinazzi R, Albertin G, Nowak M, Malendowicz L, Tortorella C, et al. Orexins stimulate glucocorticoid secretion from cultured rat and human adrenocortical cells, exclusively acting via the OX1 receptor. J Steroid Biochem Mol Biol. 2005;96:423-9 pubmed
  90. Bengtsson M, Mäkelä K, Herzig K, Flemström G. Short food deprivation inhibits orexin receptor 1 expression and orexin-A induced intracellular calcium signaling in acutely isolated duodenal enterocytes. Am J Physiol Gastrointest Liver Physiol. 2009;296:G651-8 pubmed publisher
    ..extracted from pellets of enterocytes and reverse transcribed to cDNA, and expression of orexin receptors 1 and 2 (OX1R and OX2R) was measured by quantitative real-time PCR...
  91. Ramanjaneya M, Conner A, Chen J, Stanfield P, Randeva H. Orexins stimulate steroidogenic acute regulatory protein expression through multiple signaling pathways in human adrenal H295R cells. Endocrinology. 2008;149:4106-15 pubmed publisher
    ..analysis also showed that orexin effects on StAR were primarily, but not exclusively, acting through the orexin receptor type 1. This is the first study linking orexin action on StAR expression and comprehensively describes the ..
  92. Dalrymple M, Jaeger W, Eidne K, Pfleger K. Temporal profiling of orexin receptor-arrestin-ubiquitin complexes reveals differences between receptor subtypes. J Biol Chem. 2011;286:16726-33 pubmed publisher