SB-357134

SB-357134 is a drug which is used in scientific research. It acts as a potent, selective and orally active 5-HT6 receptor antagonist.[1] SB-357134 and other 5-HT6 antagonists show nootropic effects in animal studies,[2][3][4] and have been proposed as potential novel treatments for cognitive disorders such as schizophrenia and Alzheimer's disease.

SB-357134
Identifiers
  • N-(2,5-Dibromo-3-fluorophenyl)-4-methoxy-3-(1-piperazinyl)benzenesulfonamide
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
FormulaC17H18Br2FN3O3S
Molar mass523.22 g·mol−1
3D model (JSmol)
  • C3CNCCN3c1cc(ccc1OC)S(=O)(=O)Nc2cc(Br)cc(F)c2Br
  • InChI=1S/C17H18Br2FN3O3S/c1-26-16-3-2-12(10-15(16)23-6-4-21-5-7-23)27(24,25)22-14-9-11(18)8-13(20)17(14)19/h2-3,8-10,21-22H,4-7H2,1H3 ☒N
  • Key:BLWHAZZXRHTFJE-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

References
  1. Bromidge SM, Clarke SE, Gager T, Griffith K, Jeffrey P, Jennings AJ, et al. (January 2001). "Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134)". Bioorganic & Medicinal Chemistry Letters. 11 (1): 55–8. doi:10.1016/S0960-894X(00)00597-7. PMID 11140733.
  2. Rogers DC, Hagan JJ (November 2001). "5-HT6 receptor antagonists enhance retention of a water maze task in the rat". Psychopharmacology. 158 (2): 114–9. doi:10.1007/s002130100840. PMID 11702084. S2CID 29472459.
  3. 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.
  4. Perez-García G, Meneses A (July 2005). "Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task". Pharmacology, Biochemistry, and Behavior. 81 (3): 673–82. doi:10.1016/j.pbb.2005.05.005. PMID 15964617. S2CID 19789219.
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