Effects of diltiazem on liver mitochondria of rats: a reconsideration

1. The effects of the Ca-channel blocker diltiazem (a drug of the benzothiazepine family) on bioenergetic metabolism have been assessed on isolated rat liver mitochondria. 2. Millimolar concentrations of diltiazem induced a decrease of both the ADP- and the uncoupler-stimulated respiration and a concomitant slight increase of the resting respiration. 3. Under the same experimental conditions diltiazem decreased the transmembrane electrical potential while leaving calcium uptake unaffected. 4. Micromolar concentrations of diltiazem, which are close to therapeutic haematic levels, were without effect.