SB-258,585

Из Википедије, слободне енциклопедије
SB-258,585
(IUPAC) ime
4-Jodo-N-[4-metoksi-3-(4-metil-1-piperazinil)fenil]benzensulfonamid
Klinički podaci
Identifikatori
CAS broj 209480-63-7
ATC kod nije dodeljen
PubChem[1][2] 3248571
ChEMBL[3] CHEMBL60264
Hemijski podaci
Formula C18H22IN3O3S 
Mol. masa 487,354 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

SB-258,585 je lek koji se koristi u naučnim istraživanjima. On deluje kao potentan, selektivan i oralno aktivan antagonist 5-HT6 receptora, sa Ki od 8,9 nM.[4] On se koristi u obliku 125I radio obeleženoj formi za maporamke distribucije 5-HT6 receptora u mozgu.[5][6]

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. ^ Hirst, WD; Minton, JA; Bromidge, SM; Moss, SF; Latter, AJ; Riley, G; Routledge, C; Middlemiss, DN et al. (2000). „Characterization of 125I-SB-258585 binding to human recombinant and native 5-HT6 receptors in rat, pig and human brain tissue“. British Journal of Pharmacology 130 (7): 1597–605. DOI:10.1038/sj.bjp.0703458. PMC 1572217. PMID 10928963. 
  5. ^ Roberts, JC; Reavill, C; East, SZ; Harrison, PJ; Patel, S; Routledge, C; Leslie, RA (2002). „The distribution of 5-HT(6) receptors in rat brain: an autoradiographic binding study using the radiolabelled 5-HT(6) receptor antagonist (125)ISB-258585“. Brain Research 934 (1): 49–57. DOI:10.1016/S0006-8993(02)02360-0. PMID 11937069. 
  6. ^ East, SZ; Burnet, PW; Leslie, RA; Roberts, JC; Harrison, PJ (2002). „5-HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: autoradiographic studies with 125ISB-258585“. Synapse 45 (3): 191–9. DOI:10.1002/syn.10097. PMID 12112397. 

Spoljašnje veze[уреди]