Methods for determining sodium-proton-exchanger ligand efficiency

Abstract

The present invention relates to methods for determining the efficiency of an ion channel ligand comprising (a) contacting a cell expressing the ion channel with (i) plasma of an animal and (ii) the ion channel ligand and (b) determining the effect of the ion channel ligand on the cell.

1 . A method for determining the efficiency of an ion channel ligand comprising the steps of:
 a) contacting a cell expressing the ion channel with
 i) plasma of an animal and 
 ii) the ion channel ligand; and 
   b) determining the effect of the ion channel ligand on the cell.   
     
     
         2 . The method of  claim 1 , wherein the ion channel is a Sodium-Proton-Exchanger (NHE) or a Sodium-Bicarbonate-Cotransporter. 
     
     
         3 . The method of  claim 2 , wherein the NHE is NHE1, NHE2, NHE3 or NHE5, particularly NHE1 or NHE3, especially NHE1. 
     
     
         4 . The method of  claim 1 , wherein the ion channel ligand, particularly a NHE ligand, is an agonist or an antagonist, especially NHE antagonist. 
     
     
         5 . The method of  claim 1 , wherein the cell is a cell line, particularly a mammalian cell line, particularly a human or mouse cell line, especially mouse LTK-cell line LAP1. 
     
     
         6 . The method of  claim 1 , wherein the animal is a vertebrate, particularly a mammal, especially a rat, mouse, rabbit, guinea pig, or cat. 
     
     
         7 . The method of  claim 1 , wherein the animal is a human. 
     
     
         8 . The method of  claim 1 , wherein the effect is an alteration of the pH-value. 
     
     
         9 . The method of  claim 1 , wherein the effect is an alteration of the intracellular pH-value. 
     
     
         10 . The method of  claim 1 , wherein the effect is determined by fluorescence. 
     
     
         11 . The method of  claim 1 , wherein the NHE ligand has been administered the animal, wherein the animal is a non-human animal. 
     
     
         12 . The method of  claim 1 , wherein the method is used in determined plasma concentration of a ligand. 
     
     
         13 . The method of  claim 1 , wherein the method is used for screening for a medicament for preventing and/or treating a disease involving ion channel dysfunction. 
     
     
         14 . The method of  claim 1 , wherein the method is used for screening for a medicament for preventing and/or treating a cardiovascular disease or cancer.