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- 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.
- Gunawardana, S.C. et al. (2008) Am. J. Physiol. 294, 1097.
- Gunawardana, S.C. et al. (2005) BMC Endocr. Disord. 5, 9.
- Soliman, M. (2009) J. Saudi Heart Assoc. 21, 159.
- Cui, X.L. et al. (2002) Sheng Li Xue Bao. 54, 219.
- Banke, T.G. (2011) Brain Res. 1381, 21.
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.
5-(N,N-Dimethyl)amiloride hydrochloride (#D-165) is a highly pure, synthetic, and biologically active compound.
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