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Synthesis and Inhibition Effects on 5-HT6 Receptor of Benzothiazole Derivatives

Authors
Hayat, Faisal; Yoo, Euna; Rhim, Hyewhon; Choo, Hea-Young Park
Issue Date
2013-02
Publisher
KOREAN CHEMICAL SOC
Citation
BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.34, no.2, pp.495 - 499
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 mu M. Compound 13 also showed good selectivity on the 5-HT6 over 5-HT4 and 5-HT7 receptors.
Keywords
CENTRAL-NERVOUS-SYSTEM; SEROTONIN RECEPTOR; MOLECULAR-CLONING; RAT; LOCALIZATION; ANTAGONISTS; LIGANDS; PHARMACOLOGY; MUTAGENESIS; PROGRESS; Sulfonamide; N-Methyl piperazine; 5-HT6 receptor antagonist
ISSN
0253-2964
URI
https://pubs.kist.re.kr/handle/201004/128375
DOI
10.5012/bkcs.2013.34.2.495
Appears in Collections:
KIST Article > 2013
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