SB-258585
Chemical compound / From Wikipedia, the free encyclopedia
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]
Quick Facts Identifiers, CAS Number ...
Identifiers | |
---|---|
| |
CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider |
|
UNII | |
ChEMBL | |
Chemical and physical data | |
Formula | C18H22IN3O3S |
Molar mass | 487.36 g·mol−1 |
3D model (JSmol) | |
| |
| |
NY (what is this?) (verify) |
Close
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.
- Hirst WD, Minton JA, Bromidge SM, Moss SF, Latter AJ, Riley G, et al. (August 2000). "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. doi:10.1038/sj.bjp.0703458. PMC 1572217. PMID 10928963.
- Roberts JC, Reavill C, East SZ, Harrison PJ, Patel S, Routledge C, Leslie RA (April 2002). "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. doi:10.1016/S0006-8993(02)02360-0. PMID 11937069. S2CID 140209933.
- Stean TO, Hirst WD, Thomas DR, Price GW, Rogers D, Riley G, et al. (April 2002). "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. doi:10.1016/S0091-3057(01)00742-0. PMID 11888556. S2CID 34925312.
- Wesołowska A, Nikiforuk A, Stachowicz K (September 2007). "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. doi:10.1097/FBP.0b013e3282d28f9c. PMID 17762512. S2CID 20105974.
This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it. |