Abstract
This paper describes the inhibitory effects of several antianginal drugs on 22Na uptake of the fast Na + channel in rat brain synaptosomes and in rat heart muscle cells in culture. Calcium antagonists like verpamil, flunarizine, perhexiline, two perhexiline derivatives IPS 629 and IPS 672, and β-adrenoceptor antagonists like propranolol and practolol were tested. IPS 672 was the most active compound on synaptosomes and heart muscle cells IC 50 = 2.0 × 10 −6 and 2.4 × 10 −6 M respectively). The relative potencies of the Ca 2+ antagonists tested on heart muscle cells were found to be IPS 672 > IPS 629 > perhexiline > flunarizine > verapamil. Verapamil was 55 and 10 times less active than IPS 672 on synaptosomes and heart cells respectively. Propranolol had an inhibitory activity comparable to that of flunarizine and was 100 times more active than practolol. It can be concluded that several antianginal drugs seem to interfere with the Na + fast channel on rat brain and heart.
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