Na/Ca exchange and tension development in vascular smooth muscle: effect of amiloride.

1. The potassium-sparing diuretic, amiloride, has been shown to inhibit the Na/Ca exchange system in various preparations. The effects of this drug have been investigated on the contractions of guinea-pig aortic strips elicited by reduction of external K, by addition of ouabain and by removal of external Na. 2. Amiloride (5 X 10(-6) M-5 X 10(-4) M) inhibited the mechanical responses when it was added before giving the stimulus for contractions, but was not effective in relaxing the contracted strips. The drug shifted to the right the dose-response curve for Ca in low K solution. 3. The calcium antagonist diltiazem had no effect on the ouabain-, low K- and Na-free-induced contractions. 4. Amiloride decreased the rate of relaxation of aortic strips induced by removal of the low K solution. 5. The pattern of amiloride action on ouabain-, low K- and Na-free-induced contractions suggests that the drug interferes with Ca influx. The effect of amiloride on the relaxation rate of low K-contracted aortic strips is consistent with an interference with Ca efflux. 6. It is suggested that amiloride prevents Ca fluxes through the Na/Ca exchange system of guinea-pig aortic strips.