Novel far-red fluorescent 1,4-dihydropyridines for L-type calcium channels imaging

07 November 2023, Version 1

Abstract

Upregulation of L-type calcium channels (LTCCs) is implicated in a range of cardiovascular and neurological disorders. Therefore, the development of toolboxes that unlocks fast imaging protocols in live cells are coveted. Herein, we report a library of first-in-class novel far-red small-molecule-based fluorescent ligands (FluoDiPines), able to target LTCCs. All fluorescent ligands were evaluated in whole-cell patch-clamp and live-cell Ca2+ imaging whereby Fluodipine 6 was found the best candidate for live-cell fluorescence imaging. Low concentration of FluoDiPine 6 (50 nM) and a quick labelling protocol (5 min) are successfully applied to fixed- and live-cells to image LTCCs with good specificity.

Keywords

L-type calcium channels
Ion channels
Live-cell imaging
Confocal
Fluorescence imaging
Calcium channel blockers

Supplementary materials

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Supplementary materials
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Supporting information includes: biological protocols, synthetic protocols and compound characterization.
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