Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands.

Authors :: 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
Source :: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2011 Nov 15; Vol. 19 (22), pp. 6750-9. Date of Electronic Publication: 2011 Sep 29.
Publication Year :: 2011
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.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)