5-(N,N-Dimethyl)amiloride hydrochloride

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 absent^1,2. 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.