Catalog Number: 1960
Chemical Name: N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea
Biological Activity
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
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO with gentle warming and to 10 mM in ethanol with gentle warming
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline
Background References
  1. 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
  2. A selective orexin-1 receptor antagonist reduces food consumption in male and female rats.
    Haynes et al.
    Regul.Pept., 2000;96:45
  3. SB-334867-A: the first selective orexin-1 receptor antagonist.
    Smart et al.
    Br.J.Pharmacol., 2001;132:1179
  4. 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.
    Porter et al.
    Bioorg.Med.Chem.Lett., 2001;11:1907

The citations listed below are publications that use Tocris products. Selected citations for SB 334867 include:

Showing Results 1 - 10 of 25

  1. Antagonistic interplay between hypocretin and leptin in the lateral hypothalamus regulates stress responses.
    Authors: Bonnavion Et al.
    Nat Commun
  2. Perifornical hypothalamic orexin and serotonin modulate the counterregulatory response to hypoglycemic and glucoprivic stimuli.
    Authors: Otlivanchik Et al.
    Neurosci Lett
  3. 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
  4. Orexin-corticotropin-releasing factor receptor heteromers in the ventral tegmental area as targets for cocaine.
    Authors: Navarro Et al.
  5. Orexinergic neurotransmission in temperature responses to methamphetamine and stress: mathematical modeling as a data assimilation approach.
    Authors: Behrouzvaziri Et al.
    PLoS One
  6. 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
  7. Acute high fat diet consumption activates the mesolimbic circuit and requires orexin signaling in a mouse model.
    Authors: Valdivia Et al.
    PLoS One
  8. 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
  9. The hypocretin/orexin system mediates the extinction of fear memories.
    Authors: Flores Et al.
  10. Attenuated orexinergic signaling underlies depression-like responses induced by daytime light deficiency.
    Authors: Deats Et al.
  11. Orexin A Affects INS-1 Rat Insulinoma Cell Proliferation via Orexin Receptor 1 and the AKT Signaling Pathway.
    Authors: Chen Et al.
    Int J Endocrinol
  12. Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery.
    Authors: Putula Et al.
    Br J Pharmacol
  13. 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
  14. A role for hypocretin/orexin receptor-1 in cue-induced reinstatement of nicotine-seeking behavior.
    Authors: Plaza-Zabala Et al.
  15. 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
  16. 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
  17. Involvement of spinal orexin A in the electroacupuncture analgesia in a rat model of post-laparotomy pain.
    Authors: Feng Et al.
    Brain Res
  18. Orexin 1 receptors are a novel target to modulate panic responses and the panic brain network.
    Authors: Johnson Et al.
    Sci Rep
  19. 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
  20. 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
  21. Orexins/hypocretins act in the posterior paraventricular thalamic nucleus during repeated stress to regulate facilitation to novel stress.
    Authors: Heydendael Et al.
  22. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor.
    Authors: Malherbe Et al.
    Br J Pharmacol
  23. Role of orexin input in the diurnal rhythm of locus coeruleus impulse activity.
    Authors: Gompf and Aston-Jones
  24. Insular hypocretin transmission regulates nicotine reward.
    Authors: Hollander Et al.
    Proc Natl Acad Sci U S A
  25. Orexin A induces GnRH gene expression and secretion from GT1-7 hypothalamic GnRH neurons.
    Authors: Sasson Et al.
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