Pharmacological profile of SB-357134: A potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist

@article{Stean2002PharmacologicalPO,
  title={Pharmacological profile of SB-357134: A potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist},
  author={Tania O. Stean and Warren D. Hirst and David R. Thomas and Gary W. Price and Derek C. Rogers and Graham J. Riley and Steven Mark Bromidge and Halina T. Serafinowska and Douglas R Smith and Sarah Bartlett and Nigel J. Deeks and Mark S. Duxon and Neil Upton},
  journal={Pharmacology Biochemistry and Behavior},
  year={2002},
  volume={71},
  pages={645-654}
}
N-(2,5-Dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134) potently inhibited [125I]SB-258585 and [3H]LSD binding in a HeLa cell line expressing human 5-HT(6) receptors (pK(i)=8.6 and 8.54, respectively). Furthermore, SB-357134 inhibited [125I]SB-258585 binding in human caudate--putamen and in rat and pig striatum membranes (pK(i)=8.82, 8.44, and 8.61, respectively). SB-357134 displayed over 200-fold selectivity for the 5-HT(6) receptor versus 72 other receptors and… Expand
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