Several compounds with a 4-aminopiperidine scaffold decorated on both nitrogen atoms by alkyl or acyl moieties containing the structural motifs of verapamil and of flunarizine, as well as those that are more frequent in known N-type calcium channel antagonists, have been synthesized. Antinociceptive activity on the mouse hot-plate test was used to select molecules to be submitted to further studies. Active compounds were tested in vitro on a PC12 rat pheochromocytoma clonal cell line, to evaluate their action on N-type calcium channels, and on a rat model of neuropathic pain. Two compounds that show N-type calcium channel antagonism and are endowed with potent action on pain and neuropathic pain (3 and 18) have been selected for further studies.

Design, synthesis and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain / Teodori, Elisabetta; Baldi, Elisabetta; Dei, Silvia; Gualtieri, Fulvio; Romanelli, MARIA NOVELLA; Scapecchi, Serena; Bellucci, Cristina; Ghelardini, Carla; Matucci, Rosanna. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 47:(2004), pp. 6070-6081. [10.1021/jm049923l]

Design, synthesis and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain

TEODORI, ELISABETTA;BALDI, ELISABETTA;DEI, SILVIA;GUALTIERI, FULVIO;ROMANELLI, MARIA NOVELLA;SCAPECCHI, SERENA;BELLUCCI, CRISTINA;GHELARDINI, CARLA;MATUCCI, ROSANNA
2004

Abstract

Several compounds with a 4-aminopiperidine scaffold decorated on both nitrogen atoms by alkyl or acyl moieties containing the structural motifs of verapamil and of flunarizine, as well as those that are more frequent in known N-type calcium channel antagonists, have been synthesized. Antinociceptive activity on the mouse hot-plate test was used to select molecules to be submitted to further studies. Active compounds were tested in vitro on a PC12 rat pheochromocytoma clonal cell line, to evaluate their action on N-type calcium channels, and on a rat model of neuropathic pain. Two compounds that show N-type calcium channel antagonism and are endowed with potent action on pain and neuropathic pain (3 and 18) have been selected for further studies.
2004
47
6070
6081
Teodori, Elisabetta; Baldi, Elisabetta; Dei, Silvia; Gualtieri, Fulvio; Romanelli, MARIA NOVELLA; Scapecchi, Serena; Bellucci, Cristina; Ghelardini, Carla; Matucci, Rosanna
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/256079
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