Newly synthesized I(f) blockers demonstrate isoform selectivity for HCN1 and HCN2 channels in vitro, providing potential pharmacological tools for studying these channels.
Isoform-selective I(f) blockers may aid HCN research tools; leaves open clinical translation in cardiac disease.
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.
No takes yet. Share an insight, caveat, or question.
Melchiorre et al. (2010) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: