| Literature DB >> 22001327 |
Paweł Zajdel1, Krzysztof Marciniec, Andrzej Maślankiewicz, Maria H Paluchowska, Grzegorz Satała, Anna Partyka, Magdalena Jastrzębska-Więsek, Dagmara Wróbel, Anna Wesołowska, Beata Duszyńska, Andrzej J Bojarski, Maciej Pawłowski.
Abstract
Novel arene- and quinolinesulfonamides were synthesized using different solutions and a solid-support methodology, and were evaluated for their affinity for 5-HT(1A), 5-HT(2A), 5-HT(6), and 5-HT(7) receptors. Compound 54 (N-Ethyl-N-[4-(1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinolin-2-yl)butyl]-8-quinolinesulfonamide) was identified as potent 5-HT(7) antagonist (K(i)=13 nM, K(B)=140 nM) with good selectivity over 5-HT(1A), 5-HT(2A), 5-HT(6) receptors. In the FST in mice, it reduced immobility in a manner similar to the selective 5-HT(7) antagonist SB-269970.Entities:
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Year: 2011 PMID： 22001327 DOI： 10.1016/j.bmc.2011.09.044
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641