Format

Send to

Choose Destination
Bioorg Med Chem. 2011 Nov 15;19(22):6750-9. doi: 10.1016/j.bmc.2011.09.044. Epub 2011 Sep 29.

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

Author information

1
Department of Medicinal Chemistry, Jagiellonian University Medical College, Kraków, Poland. mfzajdel@cyf-kr.edu.pl

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.

PMID:
22001327
DOI:
10.1016/j.bmc.2011.09.044
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center