Referenced in: none

Automatically associated channels: HCN1 , HCN2 , HCN3 , HCN4

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

Authors: Michele Melchiorre, Martina Del Lungo, Luca Guandalini, Elisabetta Martini, Silvia Dei, Dina Manetti, Serena Scapecchi, Elisabetta Teodori, Laura Sartiani, Alessandro Mugelli, Elisabetta Cerbai, Maria Novella Romanelli

Journal, date & volume: J. Med. Chem., 2010 Sep 23 , 53, 6773-7

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/20795648

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.