We have previously reported on the Ca
2+-blocking activity and active constituents of natural products. In the course of screening, UNCARIAE RAMULUS ET UNCUS, a chinese herbal medicine, was found to possess such activity. In this paper, we attempted to characterize its active constituent which plays an important role in Ca
2+-blocking activity. Its active principles were identified to be oxyindole-type alkaloids, rhynchophylline, corynoxeine, isorhynchophylline and isocorynoxeine, that showed inhibitory effects, similar to that of verapamil, on contractile response to high concentration of potassium ion (rats), CaCl
2 (rats), norepinephrine in normal and Ca
2+-free medium (rats and rabbits) and
45Ca
2+-uptake (rats) in thoracic aorta with an activity two orders of magnitude less than the activity of verapamil.
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