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Published on: May 7, 2013
Novel Far-Red Fluorescent 1,4-Dihydropyridines for L-Type Calcium Channel Imaging
Carlotta Borgarelli1, Yvonne E Klingl2,3, Abril Escamilla-Ayala4,5
1Sustainable Chemistry for Metals and Molecules (SCM2), Department of Chemistry, KU Leuven, Celestijnenlaan 200F, Box 2404, 3001 Leuven, Belgium.
Abstract:
Upregulation of L-type calcium channels (LTCCs) is implicated in a range of cardiovascular and neurological disorders. Therefore, the development of toolboxes that unlock fast imaging protocols in live cells is coveted. Herein, we report a library of first-in-class 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 to be the best candidate for live-cell fluorescence imaging. Low concentration of FluoDiPine 6 (50 nM) and a quick labeling protocol (5 min) are successfully applied to fixed and live cells to image LTCCs with good specificity.

