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Submit ReviewSB 334867
Description: Selective non-peptide OX1 antagonist
Chemical Name: N-(2-Methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea
Purity: ≥99% (HPLC)
Biological Activity for SB 334867
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.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries for SB 334867
SB 334867 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SB 334867
| M. Wt | 319.32 |
| Formula | C17H13N5O2 |
| Storage | Store 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SB 334867
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.93 | 100 with gentle warming | |
| ethanol | 3.19 | 10 with gentle warming |
Preparing Stock Solutions for SB 334867
The following data is based on the product molecular weight 319.32. Batch specific molecular weights may vary from batch to batch due to the degree 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 for SB 334867
References for SB 334867
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for SB 334867, please let us know.
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Keywords: SB 334867, SB 334867 supplier, Selective, non-peptide, OX1, antagonists, Orexin1, Receptors, SB334867, GlaxoSmithKline, GSK, Receptor, 1960, Tocris Bioscience
48 Citations for SB 334867
Citations are publications that use Tocris products. Selected citations for SB 334867 include:
Hsu et al (2015) Hippocampus ghrelin signaling mediates appetite through lateral hypothalamic orexin pathways. Elife 4 PMID: 26745307
Zhou et al (2015) Upregulation of orexin receptor in paraventricular nucleus promotes sympathetic outflow in obese Zucker rats. Neuropharmacology 99 481 PMID: 26277341
Behrouzvaziri et al (2015) Orexinergic neurotransmission in temperature responses to metha. 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
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 (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
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
Soya (2017) Orexin modulates behavioral fear expression through the locus coeruleus. Nat Commun 8 1606 PMID: 29151577
Jerlhag et al (2011) Glutamatergic regulation of ghrelin-induced activation of the mesolimbic DA system. Addict Biol 16 82 PMID: 20579004
Tupone et al (2011) An orexinergic projection from perifornical hypothalamus to raphe pallidus increases rat brown adipose tissue thermogenesis. J Neurosci 31 15944 PMID: 22049437
Parise et al (2011) Evidence for the role of hindbrain orexin-1 receptors in the control of meal size. Am J Physiol Regul Integr Comp Physiol 301 R1692 PMID: 21957165
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
Prince et al (2015) Hypocretin/Orexin regulation of DA signaling and cocaine self-administration is mediated predominantly by hypocretin receptor 1. ACS Chem Neurosci 6 138 PMID: 25496218
Mahler et al (2013) Interactions between VTA orexin and glutamate in cue-induced reinstatement of cocaine seeking in rats. Psychopharmacology (Berl) 226 687 PMID: 22411428
Qi et al (2013) Orexin receptors within the nucleus accumbens shell mediate the stress but not drug priming-induced reinstatement of mor. conditioned place preference. Front Behav Neurosci 7 144 PMID: 24133421
Adidharma et al (2012) Orexinergic signaling mediates light-induced neuronal activation in the dorsal raphe nucleus. Neuroscience 220 201 PMID: 22710065
Yi et al (2012) Occurrence of epilepsy at different zeitgeber times alters sleep homeostasis differently in rats. Sleep 35 1651 PMID: 23204608
Laorden et al (2012) Hypothalamic orexin--a neurons are involved in the response of the brain stress system to mor. withdrawal. PLoS One 7 e36871 PMID: 22590628
Patyal et al (2012) Local hypocretin-1 modulates terminal DA concentration in the nucleus accumbens shell. Front Behav Neurosci 6 82 PMID: 23226119
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
Chen et al (2016) Theta synchronization between medial prefrontal cortex and cerebellum is associated with adaptive performance of associative learning behavior. Sci Rep 6 20960 PMID: 26879632
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
Riday et al (2012) Orexin-1 receptor antagonism does not reduce the rewarding potency of cocaine in Swiss-Webster mice. Brain Res 1431 53 PMID: 22133306
Srinivasan et al (2012) The dual orexin/hypocretin receptor antagonist, almorexant, in the ventral tegmental area attenuates ethanol self-administration. PLoS One 7 e44726 PMID: 23028593
España et al (2010) The hypocretin-orexin system regulates cocaine self-administration via actions on the mesolimbic DA system. Eur J Neurosci 31 336 PMID: 20039943
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
Razavi et al (2014) Chemical stimulation of the lateral hypothalamus potentiated the sensitization to mor. in rats: involvement of orexin-1 receptor in the ventral tegmental area. EXCLI J 13 1120 PMID: 26417327
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
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
Federici et al (2016) Hypothalamic orexin's role in exacerbated cutaneous vasodilation responses to an anxiogenic stimulus in a surgical menopause model. Psychoneuroendocrinology 65 127 PMID: 26765933
Chen et al (2014) Orexin A Affects INS-1 Rat Insoma 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
Shu et al (2014) Orexin-A promotes cell migration in cultured rat astrocytes via Ca2+-dependent PKCα and ERK1/2 signals. PLoS One 9 e95259 PMID: 24748172
Kay et al (2014) Hindbrain orexin 1 receptors influence palatable food intake, operant responding for food, and food-conditioned place preference in rats. Psychopharmacology (Berl) 231 419 PMID: 23978908
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
Deats et al (2014) Attenuated orexinergic signaling underlies depression-like responses induced by daytime light deficiency. Neuroscience 272 252 PMID: 24813431
Deng et al (2007) Contribution of orexin in hypercapnic chemoreflex: evidence from genetic and pharmacological disruption and supplementation studies in mice. J Appl Physiol (1985) 103 1772 PMID: 17717124
Sasson et al (2006) Orexin A induces GnRH gene expression and secretion from GT1-7 hypothalamic GnRH neurons. Neuroendocrinology 84 353 PMID: 17192702
D'Anna and Gammie (2006) Hypocretin-1 dose-dependently modulates maternal behaviour in mice. J Neuroendocrinol 18 553 PMID: 16867176
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
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