Chemistry:SB-334867

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Short description: Chemical compound
SB-334867
SB-334,867.svg
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
FormulaC17H13N5O2
Molar mass319.324 g·mol−1
3D model (JSmol)
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SB-334867 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX1, with around 50x selectivity for OX1 over OX2 receptors.[1] It has been shown to produce sedative and anorectic effects in animals,[2] and has been useful in characterising the orexinergic regulation of brain systems involved with appetite and sleep,[3][4][5][6][7][8] as well as other physiological processes.[9][10][11][12] The hydrochloride salt of SB-334867 has been demonstrated to be hydrolytically unstable, both in solution and as the solid.[13] Orexin antagonists have multiple potential clinical applications including the treatment of drug addiction, insomnia, obesity and diabetes.[14][15][16][17][18][19][20][21]

References

  1. ↑ "SB-334867-A: the first selective orexin-1 receptor antagonist". British Journal of Pharmacology 132 (6): 1179–82. March 2001. doi:10.1038/sj.bjp.0703953. PMID 11250867. 
  2. ↑ "SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats". The European Journal of Neuroscience 13 (7): 1444–52. April 2001. doi:10.1046/j.0953-816x.2001.01518.x. PMID 11298806. 
  3. ↑ "Anorectic, thermogenic and anti-obesity activity of a selective orexin-1 receptor antagonist in ob/ob mice". Regulatory Peptides 104 (1–3): 153–9. March 2002. doi:10.1016/S0167-0115(01)00358-5. PMID 11830290. 
  4. ↑ "Orexins and appetite regulation". Neuropeptides 36 (5): 303–25. October 2002. doi:10.1016/S0143-4179(02)00085-9. PMID 12450737. 
  5. ↑ "Hypocretin-1 causes G protein activation and increases ACh release in rat pons". The European Journal of Neuroscience 18 (7): 1775–85. October 2003. doi:10.1046/j.1460-9568.2003.02905.x. PMID 14622212. https://deepblue.lib.umich.edu/bitstream/2027.42/75751/1/j.1460-9568.2003.02905.x.pdf. 
  6. ↑ "Pharmacological characterisation of the orexin receptor subtype mediating postsynaptic excitation in the rat dorsal raphe nucleus". Neuropharmacology 46 (8): 1168–76. June 2004. doi:10.1016/j.neuropharm.2004.02.014. PMID 15111023. 
  7. ↑ "Orexin A in the nucleus accumbens stimulates feeding and locomotor activity". Brain Research 1050 (1–2): 156–62. July 2005. doi:10.1016/j.brainres.2005.05.045. PMID 15979595. 
  8. ↑ "Food-elicited increases in cortical acetylcholine release require orexin transmission". Neuroscience 149 (3): 499–507. November 2007. doi:10.1016/j.neuroscience.2007.07.061. PMID 17928158. 
  9. ↑ "Central orexin A has site-specific effects on luteinizing hormone release in female rats". Endocrinology 144 (7): 3225–36. July 2003. doi:10.1210/en.2002-0041. PMID 12810579. 
  10. ↑ "Hypocretin-1 dose-dependently modulates maternal behaviour in mice". Journal of Neuroendocrinology 18 (8): 553–66. August 2006. doi:10.1111/j.1365-2826.2006.01448.x. PMID 16867176. 
  11. ↑ "A role for hypocretin (orexin) in male sexual behavior". The Journal of Neuroscience 27 (11): 2837–45. March 2007. doi:10.1523/JNEUROSCI.4121-06.2007. PMID 17360905. 
  12. ↑ "Role of the ventromedial hypothalamic orexin-1 receptors in regulation of gastric Acid secretion in conscious rats". Journal of Neuroendocrinology 21 (3): 177–82. March 2009. doi:10.1111/j.1365-2826.2009.01824.x. PMID 19207823. 
  13. ↑ "Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: possible confounding effects on in vivo and in vitro studies". Bioorganic & Medicinal Chemistry Letters 22 (21): 6661–4. November 2012. doi:10.1016/j.bmcl.2012.08.109. PMID 23031594. 
  14. ↑ "Orexins and the treatment of obesity". European Journal of Pharmacology 440 (2–3): 199–212. April 2002. doi:10.1016/S0014-2999(02)01429-2. PMID 12007536. 
  15. ↑ "Eating, sleeping and rewarding: orexin receptors and their antagonists". Current Opinion in Drug Discovery & Development 9 (5): 551–9. September 2006. PMID 17002215. 
  16. ↑ "Orexin A in the VTA is critical for the induction of synaptic plasticity and behavioral sensitization to cocaine". Neuron 49 (4): 589–601. February 2006. doi:10.1016/j.neuron.2006.01.016. PMID 16476667. 
  17. ↑ "Direct involvement of orexinergic systems in the activation of the mesolimbic dopamine pathway and related behaviors induced by morphine". The Journal of Neuroscience 26 (2): 398–405. January 2006. doi:10.1523/JNEUROSCI.2761-05.2006. PMID 16407535. 
  18. ↑ "The orexin system regulates alcohol-seeking in rats". British Journal of Pharmacology 148 (6): 752–9. July 2006. doi:10.1038/sj.bjp.0706789. PMID 16751790. 
  19. ↑ "Orexin mediates the expression of precipitated morphine withdrawal and concurrent activation of the nucleus accumbens shell". Biological Psychiatry 64 (3): 175–83. August 2008. doi:10.1016/j.biopsych.2008.03.006. PMID 18423425. 
  20. ↑ "Role of lateral hypothalamic orexin neurons in reward processing and addiction". Neuropharmacology 56 (Suppl 1): 112–21. 2009. doi:10.1016/j.neuropharm.2008.06.060. PMID 18655797. 
  21. ↑ "Blockade of hypocretin receptor-1 preferentially prevents cocaine seeking: comparison with natural reward seeking". NeuroReport 25 (7): 485–8. May 2014. doi:10.1097/wnr.0000000000000120. PMID 24407199. 



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