GS 386 demonstrates calcium antagonistic actions in preclinical models of rat aorta and rabbit heart.
Preclinical calcium antagonism by GS 386 merits further development; leaves open efficacy and safety in human cardiovascular disease.
The effects of GS 386, a novel benzylisoquinoline derivative, on Ca 2+ current and vasodilatation were investigated using the single rabbit atrial myocyte and rat thoracic aorta preparations. In rabbit myocytes, the Ca 2+ current was recorded during various depolarizations for 200 ms from a holding potential of −40 mV using the whole patch‐clamp technique. Superfusion of GS 386 led to a reduction of the Ca 2+ current amplitude concentration‐dependently, in which the IC 50 value was 0.25 μM. However, the dependence of the Ca 2+ current on the membrane potential was not altered by GS 386. In rat aorta, GS 386 inhibited high K + ‐induced contractions more strongly than that induced by phenylephrine. These results indicate that GS 386 has Ca 2+ antagonistic actions in rat aorta and rabbit heart.
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Chang et al. (1994) studied this question.
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