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.[1] On se koristi u obliku 125I radio obeleženoj formi za maporamke distribucije 5-HT6 receptora u mozgu.[2][3]

SB-258,585
IUPAC ime
4-Jodo-N-[4-metoksi-3-(4-metil-1-piperazinil)fenil]benzensulfonamid
Identifikatori
CAS broj209480-63-7 ДаY
ATC kodnone
PubChemCID 3248571
ChEMBLCHEMBL60264
Hemijski podaci
FormulaC18H22IN3O3S
Molarna masa487,354 g/mol
  • C3CN(C)CCN3c1cc(ccc1OC)NS(=O)(=O)c2ccc(I)cc2

Reference

уреди
  1. ^ Hirst, WD; Minton, JA; Bromidge, SM; Moss, SF; Latter, AJ; Riley, G; Routledge, C; Middlemiss, DN; Price, GW (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. PMC 1572217 . PMID 10928963. doi:10.1038/sj.bjp.0703458. 
  2. ^ 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. PMID 11937069. doi:10.1016/S0006-8993(02)02360-0. 
  3. ^ 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. PMID 12112397. doi:10.1002/syn.10097. 

Spoljašnje veze

уреди