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

Autor: Zajdel P; Department of Medicinal Chemistry, Jagiellonian University Medical College, Kraków, Poland. mfzajdel@cyf-kr.edu.pl, Marciniec K, Maślankiewicz A, Paluchowska MH, Satała G, Partyka A, Jastrzębska-Więsek M, Wróbel D, Wesołowska A, Duszyńska B, Bojarski AJ, Pawłowski M
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2011 Nov 15; Vol. 19 (22), pp. 6750-9. Date of Electronic Publication: 2011 Sep 29.
DOI: 10.1016/j.bmc.2011.09.044
Abstrakt: 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.
(Copyright © 2011 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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