SB 334867

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Cat.No. 1960 - SB 334867 | C17H13N5O2 | CAS No. 792173-99-0
Description: Selective non-peptide OX1 antagonist
Chemical Name: N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea
Purity: ≥99% (HPLC)
Datasheet
Citations (25)
Literature

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

Compound Libraries

SB 334867 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 319.32
Formula C17H13N5O2
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 792173-99-0
PubChem ID 6604926
InChI Key AKMNUCBQGHFICM-UHFFFAOYSA-N
Smiles CC1=NC2=CC=C(NC(=O)NC3=CC=NC4=CC=CN=C34)C=C2O1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 31.93 100mM with gentle warming
ethanol 3.19 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 319.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.13 mL 15.66 mL 31.32 mL
5 mM 0.63 mL 3.13 mL 6.26 mL
10 mM 0.31 mL 1.57 mL 3.13 mL
50 mM 0.06 mL 0.31 mL 0.63 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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


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

25 Citations for SB 334867

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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


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