Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Synthesis and Inhibition Effects on 5-HT6 Receptor of Benzothiazole Derivatives

  • Hayat, Faisal (College of Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University) ;
  • Yoo, Euna (College of Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University) ;
  • Rhim, Hyewhon (Center for Neuroscience, Korea Institute of Science & Technology) ;
  • ParkChoo, Hea-Young (College of Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University)
  • Received : 2012.10.22
  • Accepted : 2012.11.19
  • Published : 2013.02.20
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Abstract

A novel series of aryl sulfonylpiperazine derivatives (5-15) were synthesized as 5-$HT_6$ ligands. In vitro assay was evaluated by measuring the 5-HT-induced $Ca^{2+}$ increases using HeLa cell line expressing the cloned human 5-$HT_6$ receptor, and the compound 13 showed potent 5-$HT_6$ receptor antagonistic effect with $IC_{50}$ value of 3.9 ${\mu}M$. Compound 13 also showed good selectivity on the 5-$HT_6$ over 5-$HT_4$ and 5-$HT_7$ receptors.

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References

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