Document Report Card

ID: ALA1250521

Journal: J Med Chem

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

Authors: Melchiorre M, Del Lungo M, Guandalini L, Martini E, Dei S, Manetti D, Scapecchi S, Teodori E, Sartiani L, Mugelli A, Cerbai E, Romanelli MN.

Abstract: New I(f) 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.

CiteXplore: 20795648

DOI: 10.1021/jm1006758