SB-334,867

Из Википедије, слободне енциклопедије
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[уреди]

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  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. ^ Smart, D; Sabido-David, C; Brough, SJ; Jewitt, F; Johns, A; Porter, RA; Jerman, JC (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. PMC 1572677. PMID 11250867. 
  6. ^ Rodgers, RJ; Halford, JC; Nunes De Souza, RL; Canto De Souza, AL; Piper, DC; Arch, JR; Upton, N; Porter, RA et al. (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. ^ Haynes, AC; Chapman, H; Taylor, C; Moore, GB; Cawthorne, MA; Tadayyon, M; Clapham, JC; Arch, JR (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. ^ Rodgers, RJ; Ishii, Y; Halford, JC; Blundell, JE (2002). „Orexins and appetite regulation“. Neuropeptides 36 (5): 303–25. PMID 12450737. 
  9. ^ Bernard, R; Lydic, R; Baghdoyan, HA (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. 
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  11. ^ Thorpe, AJ; Kotz, CM (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. ^ Frederick-Duus, D; Guyton, MF; Fadel, J (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. ^ Small, CJ; Goubillon, ML; Murray, JF; Siddiqui, A; Grimshaw, SE; Young, H; Sivanesan, V; Kalamatianos, T et al. (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. ^ D'anna, KL; Gammie, SC (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. PMC 2275401. PMID 16867176. 
  15. ^ Muschamp, JW; Dominguez, JM; Sato, SM; Shen, RY; Hull, EM (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. ^ Eliassi, A; Nazari, M; Naghdi, N (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. ^ Smart, D; Haynes, AC; Williams, G; Arch, JR (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. ^ Bingham, MJ; Cai, J; Deehan, MR (2006). „Eating, sleeping and rewarding: orexin receptors and their antagonists“. Current opinion in drug discovery & development 9 (5): 551–9. PMID 17002215. 
  19. ^ Borgland, SL; Taha, SA; Sarti, F; Fields, HL; Bonci, A (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. ^ Narita, M; Nagumo, Y; Hashimoto, S; Narita, M; Khotib, J; Miyatake, M; Sakurai, T; Yanagisawa, M et al. (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. ^ Lawrence, AJ; Cowen, MS; Yang, HJ; Chen, F; Oldfield, B (2006). „The orexin system regulates alcohol-seeking in rats“. British journal of pharmacology 148 (6): 752–9. DOI:10.1038/sj.bjp.0706789. PMC 1617074. PMID 16751790. 
  22. ^ Sharf, R; Sarhan, M; Dileone, RJ (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. PMC 2529153. PMID 18423425. 
  23. ^ Aston-Jones, G; Smith, RJ; Moorman, DE; Richardson, KA (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. PMC 2635332. PMID 18655797. 

Spoljašnje veze[уреди]



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