AI Article Synopsis
- - New I(f) blockers have been developed and tested on specific cells (HEK293) to identify compounds that can selectively target different HCN channel isoforms (HCN1, HCN2, HCN4).
- - The compound (R)-5, a cis-butene derivative, shows a preference for HCN2, while another compound (R)-6, a pseudodimeric product, selectively targets HCN1.
- - These findings could be crucial for pharmacological research and the creation of safer drugs that specifically interact with these ion channels in native tissues.
Article 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.
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| http://dx.doi.org/10.1021/jm1006758 | DOI Listing |
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