1360684-66-7Relevant articles and documents
Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor - 5-HT1A/5-HT2A/5-HT7 and D 2/D3/D4 - Agents: The synthesis and pharmacological evaluation
Zajdel, Pawe?,Marciniec, Krzysztof,Ma?lankiewicz, Andrzej,Sata?a, Grzegorz,Duszyńska, Beata,Bojarski, Andrzej J.,Partyka, Anna,Jastrzbska-Wisek, Magdalena,Wróbel, Dagmara,Weso?owska, Anna,Paw?owski, MacIej
experimental part, p. 1545 - 1556 (2012/04/17)
Two series of arylpiperazinyl-alkyl quinoline-, isoquinoline-, naphthalene-sulfonamides with flexible (13-26) and semi-rigid (33-36) alkylene spacer were synthesized and evaluated for 5-HT1A, 5-HT2A, 5-HT6, 5-HT7 and selected compounds for D2, D3, D4 receptors. The compounds with a mixed 5-HT and D receptors profile 16 (N-{4-[4-(3-chlorophenyl)-piperazin-1-yl]-butyl}-3- quinolinesulfonamide) and 36 (4-(4-{2-[4-(4-chloro-phenyl)-piperazin-1-yl]- ethyl}-piperidine-1-sulfonyl)-isoquinoline), displaying antagonistic activity at 5-HT7, 5-HT2A, D2 postsynaptic sites, produced antidepressant-like effects in the forced swim test in mice and showed significant anxiolytic activity in the plus-maze test in rats. The lead compound 36, a multi-receptor 5-HT2A/5-HT7/D2/D 3/D4 agent, also displayed significant antipsychotic properties in the MK-801-induced hyperlocomotor activity in mice.