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Systematic (IUPAC) name
CAS Number 209480-63-7
PubChem CID 3248571
Chemical data
Formula C18H22IN3O3S
Molar mass 487.354 g/mol[[Script error: No such module "String".]]
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SB-258,585 is a drug which is used in scientific research. It acts as a potent, selective and orally active 5-HT6 receptor antagonist, with a Ki of 8.9nM.[1] It is used in its 125I radiolabelled form to map the distribution of 5-HT6 receptors in the brain.[2][3]

SB-258,585 and other 5-HT6 antagonists show nootropic effects in animal studies,[4][5] as well as antidepressant and anxiolytic effects,[6] and have been proposed as potential novel treatments for cognitive disorders such as schizophrenia and Alzheimer's disease.


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  1. Hirst WD, Minton JA, Bromidge SM, Moss SF, Latter AJ, Riley G, Routledge C, Middlemiss DN, Price GW. Characterization of [(125)I]-SB-258585 binding to human recombinant and native 5-HT(6) receptors in rat, pig and human brain tissue. British Journal of Pharmacology. 2000 Aug;130(7):1597-605. PMID 10928963
  2. Roberts JC, Reavill C, East SZ, Harrison PJ, Patel S, Routledge C, Leslie RA. The distribution of 5-HT(6) receptors in rat brain: an autoradiographic binding study using the radiolabelled 5-HT(6) receptor antagonist [(125)I]SB-258585. Brain Research. 2002 Apr 26;934(1):49-57. PMID 11937069
  3. East SZ, Burnet PW, Leslie RA, Roberts JC, Harrison PJ. 5-HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: autoradiographic studies with [125I]SB-258585. Synapse. 2002 Sep 1;45(3):191-9. PMID 12112397
  4. Stean TO, Hirst WD, Thomas DR, Price GW, Rogers D, Riley G, Bromidge SM, Serafinowska HT, Smith DR, Bartlett S, Deeks N, Duxon M, Upton N. Pharmacological profile of SB-357134: a potent, selective, brain penetrant, and orally active 5-HT(6) receptor antagonist. Pharmacology, Biochemistry and Behaviour. 2002 Apr;71(4):645-54. PMID 11888556
  5. Loiseau F, Dekeyne A, Millan MJ. Pro-cognitive effects of 5-HT6 receptor antagonists in the social recognition procedure in rats: implication of the frontal cortex. Psychopharmacology (Berlin). 2008 Jan;196(1):93-104. PMID 17922111
  6. Wesołowska A, Nikiforuk A, Stachowicz K. Anxiolytic-like and antidepressant-like effects produced by the selective 5-HT6 receptor antagonist SB-258585 after intrahippocampal administration to rats. Behavioural Pharmacology. 2007 Sep;18(5-6):439-46. PMID 17762512