@article {Schellenberg251, author = {G D Schellenberg and L Anderson and P D Swanson}, title = {Inhibition of Na+-Ca2+ exchange in rat brain by amiloride.}, volume = {24}, number = {2}, pages = {251--258}, year = {1983}, publisher = {American Society for Pharmacology and Experimental Therapeutics}, abstract = {Amiloride (N-amidino-3,5-diamino-6-chloropyrazine carboxamide) reversibly inhibits Na+-dependent 45Ca2+ uptake (Na+-Ca2+ exchange) by plasmalemma-enriched vesicles prepared from microsomes of rat cerebral cortex and by vesicles from osmotically shocked synaptosomes. The drug inhibits Na+-dependent Ca2+ uptake in a competitive manner with a KI of 0.25-0.34 mM. Na+-dependent 45Ca2+ efflux from vesicles is also inhibited by extravesicular amiloride. The drug does not appear to affect nonmitochondrial ATP-dependent Ca2+ transport in these vesicle preparations. Membranes containing Na+-Ca2+ carrier can be solubilized in Na+-cholate and reconstituted into phospholipid vesicles. Na+-dependent Ca2+ uptake by the vesicles is inhibited by amiloride.}, issn = {0026-895X}, URL = {https://molpharm.aspetjournals.org/content/24/2/251}, eprint = {https://molpharm.aspetjournals.org/content/24/2/251.full.pdf}, journal = {Molecular Pharmacology} }