The diuretic agent amiloride is used for the treatment of high blood pressure. LMU researchers have now synthesized a photosensitive version, which allows regulating the function of sodium-specific ion channels with light. Diuretics are pharmacological agents that increase the output of urine and are commonly used for the treatment of hypertension and heart failure. One of the best known potassium sparing diuretics – amiloride – blocks the action of so-called epithelial sodium channels (ENaCs), which have diverse physiological functions. ENaCs are heterotrimeric proteins that form channels in the cell membrane and allow the passage of sodium ions (Na+). In the kidney, the so-called alpha/beta/gamma subtype is involved in the resorption of sodium from the urine, which reduces water loss and maintains blood volume. In addition, ENaCs have been identified in non-epithelial tissue, for instance neurons, where their function is not as well understood. A team led by Dirk Trauner, Professor of Chemical Biology and Genetics at LMU, in collaboration with colleagues at Justus Liebig University in Giessen, has now modified the structure of amiloride in such a way that its action of blocking ENaCs can be controlled with light. This provides the first optical tool for an amiloride-sensitive ion channel. “The
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