Jump to main content
Jump to site search

Issue 7, 2015
Previous Article Next Article

Arylsulfonamide derivatives of (aryloxy)ethylpiperidines as selective 5-HT7 receptor antagonists and their psychotropic properties

Author affiliations

Abstract

A series of alkyl/arylsulfonamide derivatives of (aryloxy)ethylpiperidines as highly potent 5-HT7 receptor antagonists has been developed through structure-based design on the previously identified compound PZ-766. This resulted in highly potent antagonist10 (3-fluoro-N-(1-{2-[(propan-2-yl)phenoxy]ethyl}piperidin-4-yl)-benzenesulfonamide) which was more active in vivo than PZ-766 and SB-269970 in forced swim test in mice (MED = 2.5 mg kg−1), and displayed comparable effects to SB-269970 in four-plate test in mice (MED = 1.25 mg kg−1) and novel object recognition test in rats (MED = 1 mg kg−1). The results highlight the antidepressant, anxiolytic and pro-cognitive potential of the arylsulfonamide derivatives of (aryloxy)ethylpiperidines with 5-HT7 receptor antagonist properties and warrant further studies to explore their therapeutic potential for the treatment of CNS disorders.

Graphical abstract: Arylsulfonamide derivatives of (aryloxy)ethylpiperidines as selective 5-HT7 receptor antagonists and their psychotropic properties

Back to tab navigation

Supplementary files

Publication details

The article was received on 21 Apr 2015, accepted on 18 May 2015 and first published on 19 May 2015


Article type: Concise Article
DOI: 10.1039/C5MD00166H
Citation: Med. Chem. Commun., 2015,6, 1272-1277
  •   Request permissions

    Arylsulfonamide derivatives of (aryloxy)ethylpiperidines as selective 5-HT7 receptor antagonists and their psychotropic properties

    P. Zajdel, V. Canale, A. Partyka, K. Marciniec, R. Kurczab, G. Satała, A. Siwek, M. Jastrzębska-Więsek, A. Wesołowska, T. Kos, P. Popik and A. J. Bojarski, Med. Chem. Commun., 2015, 6, 1272
    DOI: 10.1039/C5MD00166H

Search articles by author

Spotlight

Advertisements