Effects of various antianginal drugs on sodium influx in rat brain synaptosomes and in rat heart muscle cells in culture.
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 verapamil, flunarizine, perhexiline, two perhexiline derivatives IPS 629 and IPS 672, and beta-adrenoceptor antagonists like propranolol and practolol were tested. IPS 672 was the most active compound on synaptosomes and heart muscle cells (IC50 = 2.0 X 10(-6) and 2.4 X 10(-6) M respectively). The relative potencies of the Ca2+ antagonists tested on heart muscle cells were found to be IPS 672 greater than IPS 629 greater than perhexiline greater than flunarizine greater than 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 seems to interfere with the Na+ fast channel on rat brain and heart.
D000787:Angina Pectoris / Q000188:drug therapy*; D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects*; D002317:Cardiovascular Agents / Q000494:pharmacology* / Q000627:therapeutic use; D002478:Cells, Cultured; D066298:In Vitro Techniques; D008297:Male; D009206:Myocardium / Q000378:metabolism*; D009498:Neurotoxins / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D012964:Sodium / Q000378:metabolism*; D012979:Sodium Radioisotopes; D013574:Synaptosomes / Q000378:metabolism*
D002317:Cardiovascular Agents; D009498:Neurotoxins; D012979:Sodium Radioisotopes; D012964:Sodium