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Examination of 5-HT6 receptor affinity in the group of arylsulfonamide derivatives

Ryszard Bugno ,  Grzegorz Satała ,  Beata Duszyńska ,  Rafał J. Kurczab ,  Andrzej J. Bojarski 

Institute of Pharmacology Polish Academy of Sciences, Department of Medicinal Chemistry, Smętna 12, Kraków 31-343, Poland

Abstract

According to the recent research studies 5-HT6 receptors have gained special interest as a drug targets for diseases such as Alzheimer's disease, anxiety/depression and schizophrenia.
This stimulated an intensive research and several new compounds have been developed as a 5-HT6 agents. Due to the arylsulfonyl moiety was a common feature of nearly all published structures, it was proposed that it constitute an important pharmacophoric element, which can influence 5-HT6 affinity. Therefore a series of arylsulfonamide derivatives (2) recently developed as 5-HT7 ligands, were examined additionally at 5-HT6 receptors. The results of receptor binding experiments revealed that the tested compounds displayed a broad range of affinity for 5-HT6 receptor (Ki = 43 – >10 000 nM) and diverse selectivity with respect to other monoamine receptors.

This study was partly supported by a grant PNRF-103-AI-1/07 from Norway through the Norwegian Financial Mechanism.

 

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Submitted: 2010-03-15 22:18
Revised:   2010-03-16 11:00