Intracellular Ca2+ release by flufenamic acid and other blockers of the non-selective cation channel.
We report in this paper using measurement of intracellular free Ca2+ with fura-2, that flufenamic acid and several related blockers of the 25 pS Ca(2+)-activated non-selective cation channel cause release of Ca2+ from an intracellular store other than the endoplasmic reticulum, possibly from mitochondria. A new compound, 4'-methyl-DPC, is found to be as effective in blocking non-selective cation channels as other flufenamate analogs but, like the parent compound, the non-selective cation channel blocker DPC, it does not cause release of Ca2+ from intracellular stores. DPC and 4'-methyl-DPC are thus the most suitable of the available blockers of non-selective cation channels for use in studies on the role of these channels in normal cell function.
Department of Physiology, University of Sydney, NSW, Australia.
P
P
Poronnik
M C
MC
Ward
D I
DI
Cook
D000818:Animals; D000831:Animals, Newborn; D002118:Calcium / Q000378:metabolism*; D002460:Cell Line; D005439:Flufenamic Acid / Q000494:pharmacology*; D007473:Ion Channels / Q000378:metabolism*; D008528:Mefenamic Acid / Q000494:pharmacology; D051379:Mice; D015394:Molecular Structure; D009544:Niflumic Acid / Q000494:pharmacology
D007473:Ion Channels; D008528:Mefenamic Acid; D009544:Niflumic Acid; D005439:Flufenamic Acid; D002118:Calcium