Optical control of L-type Ca(2+) channels using a diltiazem photoswitch
Fehrentz T., Huber FME., Hartrampf N., Bruegmann T., Frank JA., Fine NHF., Malan D., Danzl JG., Tikhonov DB., Sumser M., Sasse P., Hodson DJ., Zhorov BS., Klocker N., Trauner D.
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.