title: Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands.
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.
authors: Department of Medicinal Chemistry, Jagiellonian University Medical College, Kraków, Poland. mfzajdel@cyf-kr.edu.pl
authors: Paweł
authors: P
authors: Zajdel
authors: Krzysztof
authors: K
authors: Marciniec
authors: Andrzej
authors: A
authors: Maślankiewicz
authors: Maria H
authors: MH
authors: Paluchowska
authors: Grzegorz
authors: G
authors: Satała
authors: Anna
authors: A
authors: Partyka
authors: Magdalena
authors: M
authors: Jastrzębska-Więsek
authors: Dagmara
authors: D
authors: Wróbel
authors: Anna
authors: A
authors: Wesołowska
authors: Beata
authors: B
authors: Duszyńska
authors: Andrzej J
authors: AJ
authors: Bojarski
authors: Maciej
authors: M
authors: Pawłowski
mesh_terms: D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D001667:Binding, Competitive; D006801:Humans; D007700:Kinetics; D008024:Ligands; D008124:Locomotion / Q000187:drug effects; D008297:Male; D051379:Mice; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D051381:Rats; D011985:Receptors, Serotonin / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology
chemical_list: D000928:Antidepressive Agents; D008024:Ligands; D011804:Quinolines; D011985:Receptors, Serotonin; D013449:Sulfonamides; C104425:serotonin 7 receptor