SB-399,885

Из Википедије, слободне енциклопедије
SB-399,885
(IUPAC) ime
N-(3,5-Dihloro-2-metoksifenil)-4-metoksi-3-(1-piperazinil)benzensulfonamid
Klinički podaci
Identifikatori
CAS broj 402713-80-8
ATC kod nije dodeljen
PubChem[1][2] 6918649
ChEMBL[3] CHEMBL1210710 YesY
Hemijski podaci
Formula C18H21Cl2N3O4S 
Mol. masa 446,347 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
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Pravni status

SB-399885 je lek koji se koristi u naučnim istraživanjima. On deluje kao potentan, selektivan i oralno aktivan antagonist 5-HT6 receptora, sa Ki od 9,0 nM. SB-399885 i drugi 5-HT6 antagonisti pokazuju nootropne efekte u životinjskim studijama,[4][5] kao i antidepresivne i anksiolitičke efekte koji su uporedivi i sinergistički sa drugim lekovima kao što su imipramin i diazepam.[6][7][8] Oni potencijalno mogu da služe kao tretmani za kognitivne poremećaje, kao što je šizofrenija[9] i Alchajmerova bolest.

Reference[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. ^ 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. ^ Perez-García, G; Meneses, A (2005). „Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task“. Pharmacology, Biochemistry, and Behavior 81 (3): 673–82. DOI:10.1016/j.pbb.2005.05.005. PMID 15964617. 
  5. ^ Hirst, WD; Stean, TO; Rogers, DC; Sunter, D; Pugh, P; Moss, SF; Bromidge, SM; Riley, G et al. (2006). „SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models“. European Journal of Pharmacology 553 (1–3): 109–19. DOI:10.1016/j.ejphar.2006.09.049. PMID 17069795. 
  6. ^ Wesołowska, A; Nikiforuk, A (2007). „Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression“. Neuropharmacology 52 (5): 1274–83. DOI:10.1016/j.neuropharm.2007.01.007. PMID 17320917. 
  7. ^ Wesołowska, A (2008). „The anxiolytic-like effect of the selective 5-HT6 receptor antagonist SB-399885: the impact of benzodiazepine receptors“. European Journal of Pharmacology 580 (3): 355–60. DOI:10.1016/j.ejphar.2007.11.022. PMID 18096153. 
  8. ^ Wesołowska, A; Nikiforuk, A (2008). „The selective 5-HT(6) receptor antagonist SB-399885 enhances anti-immobility action of antidepressants in rats“. European Journal of Pharmacology 582 (1–3): 88–93. DOI:10.1016/j.ejphar.2007.12.013. PMID 18234190. 
  9. ^ Li, Z; Huang, M; Prus, AJ; Dai, J; Meltzer, HY (2007). „5-HT6 receptor antagonist SB-399885 potentiates haloperidol and risperidone-induced dopamine efflux in the medial prefrontal cortex or hippocampus“. Brain Research 1134 (1): 70–8. DOI:10.1016/j.brainres.2006.11.060. PMID 17207474. 

Spoljašnje veze[уреди]