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Recently, the anti-allergic drug tranilast has been shown to reduce the rate of coronary restenosis after percutaneous transluminal coronary angioplasty. In this study, we investigated the effect of tranilast on contraction of and Ca2+ movement in vascular smooth muscle. We measured the isometric force and fura-2-estimated intracellular Ca2+ concentrations ([Ca2+]i) of rat aortic strips. Exposure of aortic strips to tranilast (0-500 microM) dose-dependently inhibited endothelin-1-induced increases in tension and [Ca2+]i elevation of the strips. Similar inhibition by tranilast was observed in response to high K+ stimulation. These results suggest that tranilast inhibits the contraction of vascular smooth muscle by inhibiting Ca2+ mobilization, which might be related to its preventive effect on coronary restenosis after percutaneous transluminal coronary angioplasty.
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