SB 334867
Chemical Name: N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea
Purity: ≥99%
Biological Activity
SB 334867 is a selective 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Dual hypocretin receptor antagonism is more effective for sleep promotion than antagonism of either receptor alone.
Morairty SR, Revel FG, Malherbe P
PLoS ONE, 2012;7(7):e39131. -
Intramolecular fluorescence resonance energy transfer (FRET) sensors of the orexin OX1 and OX2 receptors identify slow kinetics of agonist activation.
Xu TR, Ward RJ, Pediani JD
J. Biol. Chem., 2012;287(18):14937-49. -
A selective orexin-1 receptor antagonist reduces food consumption in male and female rats.
Haynes et al.
Regul.Pept., 2000;96:45 -
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.
Psychopharmacology, 2001;153:203 -
1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.
Porter et al.
Bioorg.Med.Chem.Lett., 2001;11:1907 -
SB-334867-A: the first selective orexin-1 receptor antagonist.
Smart et al.
Br.J.Pharmacol., 2001;132:1179
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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
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Orexin modulates behavioral fear expression through the locus coeruleus.
Authors: Soya
Nat Commun 2017;8(1):1606
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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
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Hypothalamic orexin's role in exacerbated cutaneous vasodilation responses to an anxiogenic stimulus in a surgical menopause model.
Authors: Federici Et al.
Psychoneuroendocrinology 2016;65:127
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Upregulation of orexin receptor in paraventricular nucleus promotes sympathetic outflow in obese Zucker rats.
Authors: Zhou Et al.
Neuropharmacology 2015;99:481
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Antagonistic interplay between hypocretin and leptin in the lateral hypothalamus regulates stress responses.
Authors: Bonnavion Et al.
Nat Commun 2015;6:6266
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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
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Perifornical hypothalamic orexin and serotonin modulate the counterregulatory response to hypoglycemic and glucoprivic stimuli.
Authors: Otlivanchik Et al.
Neurosci Lett 2015;64:226
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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
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Hippocampus ghrelin signaling mediates appetite through lateral hypothalamic orexin pathways.
Authors: Hsu Et al.
Elife 2015;4
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Orexin-corticotropin-releasing factor receptor heteromers in the ventral tegmental area as targets for cocaine.
Authors: Navarro Et al.
Neuropsychopharmacology 2015;35:6639
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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
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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
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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
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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
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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
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The hypocretin/orexin system mediates the extinction of fear memories.
Authors: Flores Et al.
Neuropsychopharmacology 2014;39:2732
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Attenuated orexinergic signaling underlies depression-like responses induced by daytime light deficiency.
Authors: Deats Et al.
Neuroscience 2014;272:252
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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
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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
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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
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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
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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
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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
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A role for hypocretin/orexin receptor-1 in cue-induced reinstatement of nicotine-seeking behavior.
Authors: Plaza-Zabala Et al.
Diabetes 2013;38:1724
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Interactions between VTA orexin and glutamate in cue-induced reinstatement of cocaine seeking in rats.
Authors: Mahler Et al.
Psychopharmacology (Berl) 2013;226:687
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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
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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
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Local hypocretin-1 modulates terminal DA concentration in the nucleus accumbens shell.
Authors: Patyal Et al.
Front Behav Neurosci 2012;6:82
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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
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Occurrence of epilepsy at different zeitgeber times alters sleep homeostasis differently in rats.
Authors: Yi Et al.
Sleep 2012;35:1651
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Orexinergic signaling mediates light-induced neuronal activation in the dorsal raphe nucleus.
Authors: Adidharma Et al.
Neuroscience 2012;220:201
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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
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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
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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
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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
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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
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An orexinergic projection from perifornical hypothalamus to raphe pallidus increases rat brown adipose tissue thermogenesis.
Authors: Tupone Et al.
J Neurosci 2011;31:15944
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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
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Glutamatergic regulation of ghrelin-induced activation of the mesolimbic DA system.
Authors: Jerlhag Et al.
Addict Biol 2011;16:82
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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
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Orexins/hypocretins act in the posterior paraventricular thalamic nucleus during repeated stress to regulate facilitation to novel stress.
Authors: Heydendael Et al.
Endocrinology 2011;152:4738
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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
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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
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Role of orexin input in the diurnal rhythm of locus coeruleus impulse activity.
Authors: Gompf and Aston-Jones
Neuropsychopharmacology 2008;1224:43
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Insular hypocretin transmission regulates nicotine reward.
Authors: Hollander Et al.
Proc Natl Acad Sci U S A 2008;105:19480
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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
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Orexin A induces GnRH gene expression and secretion from GT1-7 hypothalamic GnRH neurons.
Authors: Sasson Et al.
Neuroendocrinology 2006;84:353
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Hypocretin-1 dose-dependently modulates maternal behaviour in mice.
Authors: D'Anna and Gammie
J Neuroendocrinol 2006;18:553
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