Influence of the absolute configuration on the vascular effects of tetrandrine and isotetrandrine in rat aorta.

The relaxant action of (1S, 1'S) tetrandrine and its isomer (1R, 1'S) isotetrandrine were examined in rat aortic strips, in presence or absence of extracellular calcium. Both alkaloids relax, concentration dependently, the contractile response elicited by depolarizing solution (KCl 80 mM) or noradrenaline (1 microM). Tetrandrine, however, showed a selectivity of action towards the KCl-induced contraction while isotetrandrine did not. In Ca(2+)-free solution, both alkaloids inhibited the contraction induced by noradrenaline, but they did not affect the transient contraction due to caffeine then this effect is not attributable to direct inhibition of the smooth muscle contractile elements. The refilling of intracellular calcium stores sensitive to noradrenaline or caffeine was significantly inhibited by both alkaloids.