Chemical Name: N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea
Biological ActivitySelective non-peptide orexin OX1 receptor antagonist. pKb values are 7.2 and < 5 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1 and OX2 receptors respectively. Blocks orexin-A induced grooming and feeding following systemic administration in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
A selective orexin-1 receptor antagonist reduces food consumption in male and female rats.
Haynes et al.
Evidence that orexin-A-evoked grooming in the rat is mediated by orexin-1 (OX1) receptors, with downstream 5-HT2C receptor involvement.
Duxon et al.
1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.
Porter et al.
SB-334867-A: the first selective orexin-1 receptor antagonist.
Smart et al.
Citations for SB 334867
The citations listed below are publications that use Tocris products. Selected citations for SB 334867 include:
48 Citations: Showing 1 - 10
Orexin modulates behavioral fear expression through the locus coeruleus.
Nat Commun 2017;8(1):1606
Theta synchronization between medial prefrontal cortex and cerebellum is associated with adaptive performance of associative learning behavior.
Authors: Chen Et al.
Sci Rep 2016;6:20960
Hypothalamic orexin's role in exacerbated cutaneous vasodilation responses to an anxiogenic stimulus in a surgical menopause model.
Authors: Federici Et al.
Upregulation of orexin receptor in paraventricular nucleus promotes sympathetic outflow in obese Zucker rats.
Authors: Zhou Et al.
Antagonistic interplay between hypocretin and leptin in the lateral hypothalamus regulates stress responses.
Authors: Bonnavion Et al.
Nat Commun 2015;6:6266
Hypocretin/Orexin regulation of DA signaling and cocaine self-administration is mediated predominantly by hypocretin receptor 1.
Authors: Prince Et al.
ACS Chem Neurosci 2015;6:138
Perifornical hypothalamic orexin and serotonin modulate the counterregulatory response to hypoglycemic and glucoprivic stimuli.
Authors: Otlivanchik Et al.
Neurosci Lett 2015;64:226
Orexin/Hypocretin-1 Receptor Antagonism Selectively Reduces Cue-Induced Feeding in Sated Rats and Recruits Medial Prefrontal Cortex and Thalamus.
Authors: Cole Et al.
J Neurosci 2015;5:16143
Hippocampus ghrelin signaling mediates appetite through lateral hypothalamic orexin pathways.
Authors: Hsu Et al.
Orexin-corticotropin-releasing factor receptor heteromers in the ventral tegmental area as targets for cocaine.
Authors: Navarro Et al.
Orexinergic neurotransmission in temperature responses to metha. and stress: mathematical modeling as a data assimilation approach.
Authors: Behrouzvaziri Et al.
PLoS One 2015;10:e0126719
Hepatic branch vagus nerve plays a critical role in the recovery of post-ischemic glucose intolerance and mediates a neuroprotective effect by hypothalamic orexin-A.
Authors: Harada Et al.
PLoS One 2014;9:e95433
Orexin-A promotes cell migration in cultured rat astrocytes via Ca2+-dependent PKCα and ERK1/2 signals.
Authors: Shu Et al.
PLoS One 2014;9:e95259
Acute high fat diet consumption activates the mesolimbic circuit and requires orexin signaling in a mouse model.
Authors: Valdivia Et al.
PLoS One 2014;9:e87478
Orexin-1 receptor mediates the increased food and water intake induced by intracerebroventricular injection of the stable somatostatin pan-agonist, ODT8-SST in rats.
Authors: Karasawa Et al.
Neurosci Lett 2014;576:88
The hypocretin/orexin system mediates the extinction of fear memories.
Authors: Flores Et al.
Attenuated orexinergic signaling underlies depression-like responses induced by daytime light deficiency.
Authors: Deats Et al.
Hindbrain orexin 1 receptors influence palatable food intake, operant responding for food, and food-conditioned place preference in rats.
Authors: Kay Et al.
Psychopharmacology (Berl) 2014;231:419
Orexin A Affects INS-1 Rat Insoma Cell Proliferation via Orexin Receptor 1 and the AKT Signaling Pathway.
Authors: Chen Et al.
Int J Endocrinol 2014;2013:854623
Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery.
Authors: Putula Et al.
Br J Pharmacol 2014;171:5816
Chemical stimulation of the lateral hypothalamus potentiated the sensitization to mor. in rats: involvement of orexin-1 receptor in the ventral tegmental area.
Authors: Razavi Et al.
EXCLI J 2014;13:1120
Circadian rhythm disruption by a novel running wheel: roles of exercise and arousal in blockade of the luteinizing hormone surge.
Authors: Duncan Et al.
Physiol Behav 2014;131:7
Orexin receptors within the nucleus accumbens shell mediate the stress but not drug priming-induced reinstatement of mor. conditioned place preference.
Authors: Qi Et al.
Front Behav Neurosci 2013;7:144
A role for hypocretin/orexin receptor-1 in cue-induced reinstatement of nicotine-seeking behavior.
Authors: Plaza-Zabala Et al.
Interactions between VTA orexin and glutamate in cue-induced reinstatement of cocaine seeking in rats.
Authors: Mahler Et al.
Psychopharmacology (Berl) 2013;226:687
The dual orexin/hypocretin receptor antagonist, almorexant, in the ventral tegmental area attenuates ethanol self-administration.
Authors: Srinivasan Et al.
PLoS One 2012;7:e44726
Hypothalamic orexin--a neurons are involved in the response of the brain stress system to mor. withdrawal.
Authors: Laorden Et al.
PLoS One 2012;7:e36871
Local hypocretin-1 modulates terminal DA concentration in the nucleus accumbens shell.
Authors: Patyal Et al.
Front Behav Neurosci 2012;6:82
Activation of the orexin 1 receptor is a critical component of CO2-mediated anxiety and hypertension but not bradycardia.
Authors: Johnson Et al.
BMC Complement Altern Med 2012;37:1911
Occurrence of epilepsy at different zeitgeber times alters sleep homeostasis differently in rats.
Authors: Yi Et al.
Orexinergic signaling mediates light-induced neuronal activation in the dorsal raphe nucleus.
Authors: Adidharma Et al.
Orexin A in rat rostral ventrolateral medulla is pressor, sympatho-excitatory, increases barosensitivity and attenuates the somato-sympathetic reflex.
Authors: Shahid Et al.
Br J Pharmacol 2012;165:2292
Orexin-1 receptor antagonism does not reduce the rewarding potency of cocaine in Swiss-Webster mice.
Authors: Riday Et al.
Brain Res 2012;1431:53
Involvement of spinal orexin A in the electroacupuncture analgesia in a rat model of post-laparotomy pain.
Authors: Feng Et al.
Brain Res 2012;12:225
Orexin 1 receptors are a novel target to modulate panic responses and the panic brain network.
Authors: Johnson Et al.
Sci Rep 2012;107:733
The role of orexin-1 receptors in physiologic responses evoked by microinjection of PgE2 or muscimol into the medial preoptic area.
Authors: Rusyniak Et al.
J Neuroinflammation 2011;498:162
An orexinergic projection from perifornical hypothalamus to raphe pallidus increases rat brown adipose tissue thermogenesis.
Authors: Tupone Et al.
J Neurosci 2011;31:15944
Evidence for the role of hindbrain orexin-1 receptors in the control of meal size.
Authors: Parise Et al.
Am J Physiol Regul Integr Comp Physiol 2011;301:R1692
Glutamatergic regulation of ghrelin-induced activation of the mesolimbic DA system.
Authors: Jerlhag Et al.
Addict Biol 2011;16:82
Intrathecal orexin A increases sympathetic outflow and respiratory drive, enhances baroreflex sensitivity and blocks the somato-sympathetic reflex.
Authors: Shahid Et al.
Br J Pharmacol 2011;162:961
Orexins/hypocretins act in the posterior paraventricular thalamic nucleus during repeated stress to regulate facilitation to novel stress.
Authors: Heydendael Et al.
The hypocretin-orexin system regulates cocaine self-administration via actions on the mesolimbic DA system.
Authors: España Et al.
Eur J Neurosci 2010;31:336
Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor.
Authors: Malherbe Et al.
Br J Pharmacol 2009;156:1326
Role of orexin input in the diurnal rhythm of locus coeruleus impulse activity.
Authors: Gompf and Aston-Jones
Insular hypocretin transmission regulates nicotine reward.
Authors: Hollander Et al.
Proc Natl Acad Sci U S A 2008;105:19480
Contribution of orexin in hypercapnic chemoreflex: evidence from genetic and pharmacological disruption and supplementation studies in mice.
Authors: Deng Et al.
J Appl Physiol (1985) 2007;103:1772
Orexin A induces GnRH gene expression and secretion from GT1-7 hypothalamic GnRH neurons.
Authors: Sasson Et al.
Hypocretin-1 dose-dependently modulates maternal behaviour in mice.
Authors: D'Anna and Gammie
J Neuroendocrinol 2006;18:553
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