New If blockers have been designed and tested on HEK293 cells stably expressing the HCN1, HCN2, and HCN4 channels to find compounds able to discriminate among the channel isoforms. Among the synthesized compounds, the cis-butene derivative (R)-5 shows some preference for HCN2 while the pseudodimeric product (R)-6 shows selectivity for HCN1. These compounds can be important pharmacological tools to study the channels in native tissues and may be useful to design safe drugs.

Design, synthesis and preliminary biological evaluation of new isoform-selective f-current blockers / M. Melchiorre; M. Del Lungo; L. Guandalini; E. Martini; S. Dei; D. Manetti; S. Scapecchi; E. Teodori; L. Sartiani; A. Mugelli; E. Cerbai; M. N. Romanelli. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 53(2010), pp. 6773-6777. [10.1021/jm1006758]

Design, synthesis and preliminary biological evaluation of new isoform-selective f-current blockers.

MELCHIORRE, MICHELE;DEL LUNGO, MARTINA;GUANDALINI, LUCA;MARTINI, ELISABETTA;DEI, SILVIA;MANETTI, DINA;SCAPECCHI, SERENA;TEODORI, ELISABETTA;SARTIANI, LAURA;MUGELLI, ALESSANDRO;CERBAI, ELISABETTA;ROMANELLI, MARIA NOVELLA
2010

Abstract

New If blockers have been designed and tested on HEK293 cells stably expressing the HCN1, HCN2, and HCN4 channels to find compounds able to discriminate among the channel isoforms. Among the synthesized compounds, the cis-butene derivative (R)-5 shows some preference for HCN2 while the pseudodimeric product (R)-6 shows selectivity for HCN1. These compounds can be important pharmacological tools to study the channels in native tissues and may be useful to design safe drugs.
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M. Melchiorre; M. Del Lungo; L. Guandalini; E. Martini; S. Dei; D. Manetti; S. Scapecchi; E. Teodori; L. Sartiani; A. Mugelli; E. Cerbai; M. N. Romanelli
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2158/394662
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