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http://dx.doi.org/10.5012/bkcs.2013.34.2.495

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)
Publication Information
Bulletin of the Korean Chemical Society / v.34, no.2, 2013 , pp. 495-499 More about this Journal
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.
Keywords
Sulfonamide; N-Methyl piperazine; 5-$HT_6$ receptor antagonist;
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