Overview
- Banke, T.G. (2011) Brain Res. 1381, 21.
- Alomone Labs 5-(N,N-Dimethyl)amiloride hydrochloride inhibits allyl isothiocyanate induced calcium signal in TRPA1 expressing cells.Dose-response curve for the inhibition of human TRPA1 expressing HEK-293 cells loaded with Calcium 5 dye for changes in intracellular Ca2+ measurements. Allyl isothiocyanate (100 µM) induced calcium signal was inhibited by 50, 100 and 200µM of 5-(N,N-Dimethyl)amiloride hydrochloride (#D-165), with estimated IC50 of about 60 µM.
5-(N,N-Dimethyl)amiloride hydrochloride (DMA) is an amiloride derivative that selectively inhibits Na+/H+ exchangers in cellular membranes, resulting in the retention of H+ ions and in the decrease of intracellular pH. Amiloride derivatives are commonly used for their diuretic and antihypertensive properties.
Several studies have reported that DMA has positive effects in pancreatic β-cells on insulin release as a result of mis-regulation of intracellular pH and enhanced insulin secretion. Thus, amiloride derivatives are promising potential therapeutic agents for Type 2 Diabetes. In addition, positive effects on other cell functions have been demonstrated such as, cell membrane electrical activity, increase in intracellular Ca2+ and retention of K+1. DMA also enables glucose to induce time-dependent potentiation and enables it to occur in situations where it is normally absent1,2. Another study has suggested the possibility of DMA protection of the heart against post-resuscitation myocardial injury3.
DMA also has the ability to inhibit the Na+/Ca2+ exchanger and to increase its currents in rat cardiomyocytes. Experimental trials have showed that DMA increases calcium sensitivity in normal and hypertrophied cardiomyocytes4.
DMA also blocks TRPA1 channels5.