1. Novel Far-Red Fluorescent 1,4-Dihydropyridines for L-Type Calcium Channel Imaging.
- Author
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Borgarelli C, Klingl YE, Escamilla-Ayala A, Scarponi C, La Rovere RML, Stoklund Dittlau K, Bultynck G, Sampaolesi M, Schoenberger M, Munck S, Van Den Bosch L, De Borggraeve WM, and Ismalaj E
- Subjects
- Humans, HEK293 Cells, Patch-Clamp Techniques, Calcium metabolism, Optical Imaging, Dihydropyridines chemistry, Dihydropyridines pharmacology, Dihydropyridines chemical synthesis, Calcium Channels, L-Type metabolism, Fluorescent Dyes chemistry, Fluorescent Dyes chemical synthesis
- 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 Ca
2+ 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.- Published
- 2024
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