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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 34, Number 2
BKCSDE 34(2)
February 20, 2013

Title	Synthesis and Inhibition Effects on 5-HT₆ Receptor of Benzothiazole Derivatives
Author	Faisal Hayat, Euna Yoo, Hyewhon Rhim, Hea-Young Park Choo*
Keywords	Sulfonamide, N-Methyl piperazine, 5-HT₆ receptor antagonist
Abstract	A novel series of aryl sulfonylpiperazine derivatives (5-15) were synthesized as 5-HT6 ligands. In vitro assay was evaluated by measuring the 5-HT-induced Ca2+ increases using HeLa cell line expressing the cloned human 5-HT6 receptor, and the compound 13 showed potent 5-HT6 receptor antagonistic effect with IC50 value of 3.9 μM. Compound 13 also showed good selectivity on the 5-HT6 over 5-HT4 and 5-HT7 receptors.
Page	495 - 499
Full Text	PDF

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