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L-type Ca(2+) channels (LTCCs) play a crucial role in excitation-contraction coupling and release of hormones from secretory cells. They are targets of antihypertensive and antiarrhythmic drugs such as diltiazem. Here, we present a photoswitchable diltiazem, FHU-779, which can be used to reversibly block endogenous LTCCs by light. FHU-779 is as potent as diltiazem and can be used to place pancreatic beta-cell function and cardiac activity under optical control.

Original publication

DOI

10.1038/s41589-018-0090-8

Type

Journal article

Journal

Nat Chem Biol

Publication Date

2018

Volume

14

Pages

764 - 767

Keywords

Calcium Channels, L-Type/chemistry/*metabolism Diltiazem/chemistry/*pharmacology Fluorescent Dyes/chemistry/*pharmacology Heart/*drug effects Humans Insulin-Secreting Cells/*drug effects/metabolism Light *Optical Imaging Photochemical Processes