1245568-06-2Relevant academic research and scientific papers
ISOFORM-SELECTIVE HCN BLOCKERS
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Page/Page column 24-25, (2011/02/24)
The present invention relates to compounds of formula (I) as isoform-selective HCN blockers. In particular said compounds showed diverse capabilities of blocking selectively isoforms HCN1, HCN2 and HCN4 expressed in HEK cells. The invention further relate
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
supporting information; experimental part, p. 6773 - 6777 (2010/12/18)
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.
