SB-271,046

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SB-271,046
(IUPAC) ime
5-hloro-N-(4-metoksi-3-piperazin-1-ilfenil)-3-metil-1-benzotiofen-2-sulfonamid
Klinički podaci
Identifikatori
ATC kod nije dodeljen
PubChem[1][2] 5312149
ChEMBL[3] CHEMBL431298 DaY
Hemijski podaci
Formula C20H22ClN3O3S2 
Mol. masa 451,989 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

SB-271,046 je lek koji se koristi u naučnim istraživanjima. On je bio jedan od prvih selektivnih antagonista 5-HT6 receptora.[4] SB-271,046 je potentan i selektivan in vitro i dobrom oralnom biodostupnošću in vivo, ali ima slabu penetraciju kroz krvno moždanu barijeru, te su razvijeni poboljšani 5-HT6 antagonisti kao što su SB-357,134 i SB-399,885.[5]

SB-271,046 povišava nivoe ekscitatornih aminokiselinskih neurotransmitera glutamata i aspartata,[6] kao i dopamina i noradrenalina[7] u frontalnom korteksu i hipokampusu pacova.[8] Pokazano je da 5-HT6 antagonisti proizvode nootropne efekte u brojnim studijama na životinjama.[9][10][11] Smatrase da ovaj lekovi ove klase mogu da nađu primenu u tretmanu šizofrenije i drugih psihijatrijskih poremećaja.[12][13][14][15]

Reference[uredi | uredi kod]

  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. ↑ 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
  4. ↑ Bromidge, SM; Brown, AM; Clarke, SE; Dodgson, K; Gager, T; Grassam, HL; Jeffrey, PM; Joiner, GF i dr.. (1999). „5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist”. Journal of Medical Chemistry 42 (2): 202–5. DOI:10.1021/jm980532e. PMID 9925723. 
  5. ↑ Ahmed, M; Briggs, MA; Bromidge, SM; Buck, T; Campbell, L; Deeks, NJ; Garner, A; Gordon, L i dr.. (2005). „Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists”. Bioorganic & Medicinal Chemistry Letters 15 (21): 4867–71. DOI:10.1016/j.bmcl.2005.06.107. PMID 16143522. 
  6. ↑ Dawson, LA; Nguyen, HQ; Li, P (2000). „In vivo effects of the 5-HT6 antagonist SB-271046 on striatal and frontal cortex extracellular concentrations of noradrenaline, dopamine, 5-HT, glutamate and aspartate”. British Journal of Pharmacology 130 (1): 23–6. DOI:10.1038/sj.bjp.0703288. PMC 1572041. PMID 10780993. 
  7. ↑ Lacroix, LP; Dawson, LA; Hagan, JJ; Heidbreder, CA (2004). „5-HT6 receptor antagonist SB-271046 enhances extracellular levels of monoamines in the rat medial prefrontal cortex”. Synapse 51 (2): 158–64. DOI:10.1002/syn.10288. PMID 14618683. 
  8. ↑ Dawson, LA; Nguyen, HQ; Li, P (2001). „The 5-HT(6) receptor antagonist SB-271046 selectively enhances excitatory neurotransmission in the rat frontal cortex and hippocampus”. Neuropsychopharmacology 25 (5): 662–8. DOI:10.1016/S0893-133X(01)00265-2. PMID 11682249. 
  9. ↑ Rogers, DC; Hagan, JJ (2001). „5-HT6 receptor antagonists enhance retention of a water maze task in the rat”. Psychopharmacology 158 (2): 114–9. DOI:10.1007/s002130100840. PMID 11702084. 
  10. ↑ Foley, AG; Murphy, KJ; Hirst, WD; Gallagher, HC; Hagan, JJ; Upton, N; Walsh, FS; Regan, CM (2004). „The 5-HT(6) receptor antagonist SB-271046 reverses scopolamine-disrupted consolidation of a passive avoidance task and ameliorates spatial task deficits in aged rats”. Neuropsychopharmacology 29 (1): 93–100. DOI:10.1038/sj.npp.1300332. PMID 14571256. 
  11. ↑ Marcos, B; Chuang, TT; Gil-Bea, FJ; Ramirez, MJ (2008). „Effects of 5-HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat”. British Journal of Pharmacology 155 (3): 434–40. DOI:10.1038/bjp.2008.281. PMC 2567877. PMID 18622410. 
  12. ↑ Minabe, Y; Shirayama, Y; Hashimoto, K; Routledge, C; Hagan, JJ; Ashby Jr, CR (2004). „Effect of the acute and chronic administration of the selective 5-HT6 receptor antagonist SB-271046 on the activity of midbrain dopamine neurons in rats: an in vivo electrophysiological study”. Synapse 52 (1): 20–8. DOI:10.1002/syn.20002. PMID 14755629. 
  13. ↑ De Foubert, G; O'Neill, MJ; Zetterström, TS (2007). „Acute onset by 5-HT(6)-receptor activation on rat brain brain-derived neurotrophic factor and activity-regulated cytoskeletal-associated protein mRNA expression”. Neuroscience 147 (3): 778–85. DOI:10.1016/j.neuroscience.2007.04.045. PMID 17560041. 
  14. ↑ Marcos, B; Aisa, B; Ramírez, MJ (2008). „Functional interaction between 5-HT(6) receptors and hypothalamic-pituitary-adrenal axis: cognitive implications”. Neuropharmacology 54 (4): 708–14. DOI:10.1016/j.neuropharm.2007.11.019. PMID 18206183. 
  15. ↑ Loiseau, F; Dekeyne, A; Millan, MJ (2008). „Pro-cognitive effects of 5-HT6 receptor antagonists in the social recognition procedure in rats: implication of the frontal cortex”. Psychopharmacology 196 (1): 93–104. DOI:10.1007/s00213-007-0934-5. PMID 17922111. 

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