SB-334,867

Izvor: Wikipedia
SB-334,867
(IUPAC) ime
1-(2-methylbenzoxazol- 6-yl)- 3-[1,5]naphthyridin- 4-yl urea
Klinički podaci
Identifikatori
CAS broj 249889-64-3
ATC kod  ?
PubChem[1][2] 6604926
ChemSpider[3] 5037182
ChEMBL[4] CHEMBL291536 YesY
Hemijski podaci
Formula C17H13N5O2 
Mol. masa 319.317 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

SB-334,867 je lek koji je bio prvi ne-peptidni selektivni antagonist oreksinskog receptora, tip OX1. On je oko 50 puta selektivniji za OX1 nego OX2 receptor.[5] Bilo je pokazano da proizvodi sedativne i anoreksične efekte kod životinja,[6] i bio je koristan za karakterizaciju oreksinske regulacije moždanih sistema za apetit i san,[7][8][9][10][11][12] kao i drugih fizioloških procesesa.[13][14][15][16] Oreksinski antagonisti imaju više mogućih kliničkih primena, kao što je tretman zavisnosti od droga, insomnije, gojaznosti i dijabetesa.[17][18][19][20][21][22][23]

Literatura[uredi - уреди]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). "Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining". J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. (2001) "SB-334867-A: the first selective orexin-1 receptor antagonist". British journal of pharmacology 132 (6): 1179–82. DOI:10.1038/sj.bjp.0703953. PMID 11250867. 
  6. (2001) "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. DOI:10.1046/j.0953-816x.2001.01518.x. PMID 11298806. 
  7. (2002) "Anorectic, thermogenic and anti-obesity activity of a selective orexin-1 receptor antagonist in ob/ob mice". Regulatory peptides 104 (1-3): 153–9. DOI:10.1016/S0167-0115(01)00358-5. PMID 11830290. 
  8. (2002) "Orexins and appetite regulation". Neuropeptides 36 (5): 303–25. PMID 12450737. 
  9. (2003) "Hypocretin-1 causes G protein activation and increases ACh release in rat pons". The European journal of neuroscience 18 (7): 1775–85. DOI:10.1046/j.1460-9568.2003.02905.x. PMID 14622212. 
  10. (2004) "Pharmacological characterisation of the orexin receptor subtype mediating postsynaptic excitation in the rat dorsal raphe nucleus". Neuropharmacology 46 (8): 1168–76. DOI:10.1016/j.neuropharm.2004.02.014. PMID 15111023. 
  11. (2005) "Orexin a in the nucleus accumbens stimulates feeding and locomotor activity". Brain research 1050 (1-2): 156–62. DOI:10.1016/j.brainres.2005.05.045. PMID 15979595. 
  12. (2007) "Food-elicited increases in cortical acetylcholine release require orexin transmission". Neuroscience 149 (3): 499–507. DOI:10.1016/j.neuroscience.2007.07.061. PMID 17928158. 
  13. (2003) "Central orexin a has site-specific effects on luteinizing hormone release in female rats". Endocrinology 144 (7): 3225–36. DOI:10.1210/en.2002-0041. PMID 12810579. 
  14. (2006) "Hypocretin-1 dose-dependently modulates maternal behaviour in mice". Journal of neuroendocrinology 18 (8): 553–66. DOI:10.1111/j.1365-2826.2006.01448.x. PMID 16867176. 
  15. (2007) "A role for hypocretin (orexin) in male sexual behavior". The Journal of neuroscience : the official journal of the Society for Neuroscience 27 (11): 2837–45. DOI:10.1523/JNEUROSCI.4121-06.2007. PMID 17360905. 
  16. (2009) "Role of the ventromedial hypothalamic orexin-1 receptors in regulation of gastric Acid secretion in conscious rats". Journal of neuroendocrinology 21 (3): 177–82. DOI:10.1111/j.1365-2826.2009.01824.x. PMID 19207823. 
  17. (2002) "Orexins and the treatment of obesity". European journal of pharmacology 440 (2-3): 199–212. DOI:10.1016/S0014-2999(02)01429-2. PMID 12007536. 
  18. (2006) "Eating, sleeping and rewarding: orexin receptors and their antagonists". Current opinion in drug discovery & development 9 (5): 551–9. PMID 17002215. 
  19. (2006) "Orexin a in the VTA is critical for the induction of synaptic plasticity and behavioral sensitization to cocaine". Neuron 49 (4): 589–601. DOI:10.1016/j.neuron.2006.01.016. PMID 16476667. 
  20. (2006) "Direct involvement of orexinergic systems in the activation of the mesolimbic dopamine pathway and related behaviors induced by morphine". The Journal of neuroscience : the official journal of the Society for Neuroscience 26 (2): 398–405. DOI:10.1523/JNEUROSCI.2761-05.2006. PMID 16407535. 
  21. (2006) "The orexin system regulates alcohol-seeking in rats". British journal of pharmacology 148 (6): 752–9. DOI:10.1038/sj.bjp.0706789. PMID 16751790. 
  22. (2008) "Orexin mediates the expression of precipitated morphine withdrawal and concurrent activation of the nucleus accumbens shell". Biological psychiatry 64 (3): 175–83. DOI:10.1016/j.biopsych.2008.03.006. PMID 18423425. 
  23. (2009) "Role of lateral hypothalamic orexin neurons in reward processing and addiction". Neuropharmacology 56 Suppl 1: 112–21. DOI:10.1016/j.neuropharm.2008.06.060. PMID 18655797. 

Spoljašnje veze[uredi - уреди]


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