SB 334867

Cat. No. 1960

SB 334867 C17H13N5O2 [792173-99-0]

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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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

M.Wt:
319.32
Formula:
C17H13N5O2
Solubility:
Soluble to 100 mM in DMSO with gentle warming and to 10 mM in ethanol with gentle warming
Purity:
>99 %
Storage:
Desiccate at RT
CAS No:
792173-99-0

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Duxon et al (2001) Evidence that orexin-A-evoked grooming in the rat is mediated by orexin-1 (OX1) receptors, with downstream 5-HT2C receptor involvement. Psychopharmacology 153 203. PMID: 11205420.

Porter et al (2001) 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor. Bioorg.Med.Chem.Lett. 11 1907. PMID: 11459658.

Smart et al (2001) SB-334867-A: the first selective orexin-1 receptor antagonist. Br.J.Pharmacol. 132 1179. PMID: 11250867.

Haynes et al (2000) A selective orexin-1 receptor antagonist reduces food consumption in male and female rats. Regul.Pept. 96 45. PMID: 11102651.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for SB 334867 include:

Behrouzvaziri et al (2015) Orexinergic neurotransmission in temperature responses to methamphetamine and stress: mathematical modeling as a data assimilation approach. PLoS One 10 e0126719. PMID: 25993564.

Bonnavion et al (2015) Antagonistic interplay between hypocretin and leptin in the lateral hypothalamus regulates stress responses. Nat Commun 6 6266. PMID: 25695914.

Cole et al (2015) Orexin/Hypocretin-1 Receptor Antagonism Selectively Reduces Cue-Induced Feeding in Sated Rats and Recruits Medial Prefrontal Cortex and Thalamus. J Neurosci 5 16143. PMID: 26536818.

Navarro et al (2015) Orexin-corticotropin-releasing factor receptor heteromers in the ventral tegmental area as targets for cocaine. Neuropsychopharmacology 35 6639. PMID: 25926444.

Otlivanchik et al (2015) Perifornical hypothalamic orexin and serotonin modulate the counterregulatory response to hypoglycemic and glucoprivic stimuli. Neurosci Lett 64 226. PMID: 25114294.

Chen et al (2014) Orexin A Affects INS-1 Rat Insulinoma Cell Proliferation via Orexin Receptor 1 and the AKT Signaling Pathway. Int J Endocrinol 2013 854623. PMID: 24382962.

Deats et al (2014) Attenuated orexinergic signaling underlies depression-like responses induced by daytime light deficiency. Neuroscience 272 252. PMID: 24813431.

Duncan et al (2014) Circadian rhythm disruption by a novel running wheel: roles of exercise and arousal in blockade of the luteinizing hormone surge. Physiol Behav 131 7. PMID: 24727338.

Flores et al (2014) The hypocretin/orexin system mediates the extinction of fear memories. Neuropsychopharmacology 39 2732. PMID: 24930888.

Harada et al (2014) 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. PLoS One 9 e95433. PMID: 24759941.

Karasawa et al (2014) Orexin-1 receptor mediates the increased food and water intake induced by intracerebroventricular injection of the stable somatostatin pan-agonist, ODT8-SST in rats. Neurosci Lett 576 88. PMID: 24915296.

Putula et al (2014) Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery. Br J Pharmacol 171 5816. PMID: 25132134.

Valdivia et al (2014) Acute high fat diet consumption activates the mesolimbic circuit and requires orexin signaling in a mouse model. PLoS One 9 e87478. PMID: 24466352.

Plaza-Zabala et al (2013) A role for hypocretin/orexin receptor-1 in cue-induced reinstatement of nicotine-seeking behavior. Diabetes 38 1724. PMID: 23518606.

Feng et al (2012) Involvement of spinal orexin A in the electroacupuncture analgesia in a rat model of post-laparotomy pain. Brain Res 12 225. PMID: 23173601.

Johnson et al (2012) Activation of the orexin 1 receptor is a critical component of CO2-mediated anxiety and hypertension but not bradycardia. BMC Complement Altern Med 37 1911. PMID: 22453138.

Johnson et al (2012) Orexin 1 receptors are a novel target to modulate panic responses and the panic brain network. Sci Rep 107 733. PMID: 22554617.

Shahid et al (2012) Orexin A in rat rostral ventrolateral medulla is pressor, sympatho-excitatory, increases barosensitivity and attenuates the somato-sympathetic reflex. Br J Pharmacol 165 2292. PMID: 21951179.

Heydendael et al (2011) Orexins/hypocretins act in the posterior paraventricular thalamic nucleus during repeated stress to regulate facilitation to novel stress. Endocrinology 152 4738. PMID: 21971160.

Rusyniak et al (2011) The role of orexin-1 receptors in physiologic responses evoked by microinjection of PgE2 or muscimol into the medial preoptic area. J Neuroinflammation 498 162. PMID: 21596094.

Shahid et al (2011) Intrathecal orexin A increases sympathetic outflow and respiratory drive, enhances baroreflex sensitivity and blocks the somato-sympathetic reflex. Br J Pharmacol 162 961. PMID: 21054340.

Malherbe et al (2009) Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor. Br J Pharmacol 156 1326. PMID: 19751316.

Gompf and Aston-Jones (2008) Role of orexin input in the diurnal rhythm of locus coeruleus impulse activity. Neuropsychopharmacology 1224 43. PMID: 18614159.

Hollander et al (2008) Insular hypocretin transmission regulates nicotine reward. Proc Natl Acad Sci U S A 105 19480. PMID: 19033203.

Sasson et al (2006) Orexin A induces GnRH gene expression and secretion from GT1-7 hypothalamic GnRH neurons. Neuroendocrinology 84 353. PMID: 17192702.

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Keywords: SB 334867, supplier, Selective, non-peptide, OX1, antagonists, Orexin1, Receptors, SB334867, GlaxoSmithKline, GSK, Tocris Bioscience, OX1 Receptor Antagonist products

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