Effect of some Pteridine compounds on the Na+ + K+)-ATPase and on the cardiac glycoside receptor of human heart). 1978

E Erdmann, and W Krawietz, and P Grosshans

Pteridine compounds are known to block Na+-reabsorption and K+-secretion in epithelial cells (salivary duct of the rat), which actively transport Na+ and K+ against an electrochemical gradient. Furthermore, there have been reports on antagonistic effects of these substances in digitalis induced arrhythmias. Therefore the actions of triamterene (Jatropur, Dyrenium), the sulfuric acid ester and the methylether of p-hydroxytriamterene (OH-triamterene) and OH-triamterene on specific [3H] g-strophanthin (ouabain) binding and Na+ + K+)-ATPase activity of isolated human cardiac cell membranes were investigated. Triamterene, the sulfuric acid ester and the methylether of OH-triamterene inhibit (Na+ + K+)-ATPase activity only at very high concentrations (10(-5)--10(-4) M). OH-Triamterene does not inhibit this enzyme at concentrations lower than 10(-3) M. The specific binding of [3H] g-strophanthin to human cardiac cell membranes is inhibited half maximally at relatively high concentrations, too (10(-5)--10(-4) M). These results are rather indicative of unspecific effects due to membrane sites of action other than the (Na+ + K+)-ATPase or the cardiac glycoside receptor.

UI MeSH Term Description Entries
D009206 Myocardium The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow. Muscle, Cardiac,Muscle, Heart,Cardiac Muscle,Myocardia,Cardiac Muscles,Heart Muscle,Heart Muscles,Muscles, Cardiac,Muscles, Heart
D011188 Potassium An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
D011621 Pteridines Compounds based on pyrazino[2,3-d]pyrimidine which is a pyrimidine fused to a pyrazine, containing four NITROGEN atoms. 1,3,5,8-Tetraazanaphthalene,Pteridine,Pteridinone,Pyrazino(2,3-d)pyrimidine,Pyrazinopyrimidine,Pyrazinopyrimidines,Pyrimido(4,5-b)pyrazine,Pteridinones
D011955 Receptors, Drug Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified. Drug Receptors,Drug Receptor,Receptor, Drug
D002301 Cardiac Glycosides Cyclopentanophenanthrenes with a 5- or 6-membered lactone ring attached at the 17-position and SUGARS attached at the 3-position. Plants they come from have long been used in congestive heart failure. They increase the force of cardiac contraction without significantly affecting other parameters, but are very toxic at larger doses. Their mechanism of action usually involves inhibition of the NA(+)-K(+)-EXCHANGING ATPASE and they are often used in cell biological studies for that purpose. Cardiac Glycoside,Cardiotonic Steroid,Cardiotonic Steroids,Glycoside, Cardiac,Glycosides, Cardiac,Steroid, Cardiotonic,Steroids, Cardiotonic
D002462 Cell Membrane The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells. Plasma Membrane,Cytoplasmic Membrane,Cell Membranes,Cytoplasmic Membranes,Membrane, Cell,Membrane, Cytoplasmic,Membrane, Plasma,Membranes, Cell,Membranes, Cytoplasmic,Membranes, Plasma,Plasma Membranes
D006321 Heart The hollow, muscular organ that maintains the circulation of the blood. Hearts
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000251 Adenosine Triphosphatases A group of enzymes which catalyze the hydrolysis of ATP. The hydrolysis reaction is usually coupled with another function such as transporting Ca(2+) across a membrane. These enzymes may be dependent on Ca(2+), Mg(2+), anions, H+, or DNA. ATPases,Adenosinetriphosphatase,ATPase,ATPase, DNA-Dependent,Adenosine Triphosphatase,DNA-Dependent ATPase,DNA-Dependent Adenosinetriphosphatases,ATPase, DNA Dependent,Adenosinetriphosphatases, DNA-Dependent,DNA Dependent ATPase,DNA Dependent Adenosinetriphosphatases,Triphosphatase, Adenosine
D012964 Sodium A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23. Sodium Ion Level,Sodium-23,Ion Level, Sodium,Level, Sodium Ion,Sodium 23

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