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SB-258,585
Systematic (IUPAC) name
4-Iodo-N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]benzenesulfonamide
Identifiers
CAS number 209480-63-7
ATC code  ?
PubChem 3248571
Chemical data
Formula C 18H22IN3O3S 
Mol. mass 487.354 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

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.

References

  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
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