SB-258585 explained

SB-258585 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-258585 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.

Notes and References

1. Hirst WD, Minton JA, Bromidge SM, Moss SF, Latter AJ, Riley G, Routledge C, Middlemiss DN, Price GW . 6 . 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 . 130 . 7 . 1597–605 . August 2000 . 10928963 . 1572217 . 10.1038/sj.bjp.0703458 .
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 . 934 . 1 . 49–57 . April 2002 . 11937069 . 10.1016/S0006-8993(02)02360-0 . 140209933 .
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 . 45 . 3 . 191–9 . September 2002 . 12112397 . 10.1002/syn.10097 . 25909618 .
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 . 6 . Pharmacological profile of SB-357134: a potent, selective, brain penetrant, and orally active 5-HT(6) receptor antagonist . Pharmacology, Biochemistry, and Behavior . 71 . 4 . 645–54 . April 2002 . 11888556 . 10.1016/S0091-3057(01)00742-0 . 34925312 .
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 . 196 . 1 . 93–104 . January 2008 . 17922111 . 10.1007/s00213-007-0934-5 . 35795618 .
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 . 18 . 5–6 . 439–46 . September 2007 . 17762512 . 10.1097/FBP.0b013e3282d28f9c . 20105974 .