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Title: Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands. Author: Zajdel P, Marciniec K, Maślankiewicz A, Paluchowska MH, Satała G, Partyka A, Jastrzębska-Więsek M, Wróbel D, Wesołowska A, Duszyńska B, Bojarski AJ, Pawłowski M. Journal: Bioorg Med Chem; 2011 Nov 15; 19(22):6750-9. PubMed ID: 22001327. 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.[Abstract] [Full Text] [Related] [New Search]