[The influence of pentifylline and theophylline on reaction kinetics on rat brain ATPase stimulatable by catecholamines (author's transl)]. 1979

E Porsche, and V Stefanovich

The effects of 1-hexyl-3,7-dimethyl-xanthine (pentifylline, Cosaldon) and theophylline on rat brain Na+-, K+-, Mg2+ ATPase activities were investigated in in vitro experiments. It was established that pentifylline inhibits catecholamine sensitive ATPase in a dose dependent manner. Theophylline was without effect. Pentifylline also inhibited the Mg2+-dependent portion of Na+, K+-, Mg2+-ATPase. The effect of pentifylline on the kinetic parameters of Na+-, K+-, Mg2+-ATPase of synaptosomes was studied in detail. It was shown by a Lineweaver-Burk plot under the influence of pentifylline that the Michaelis constant (Km) increases from 1.0 x 10(-4) mol/l to 6.7 x 10(-4) mol/l. Km by norepinephrine stimulated ATPase decreases from 3.7 x 10(-4) mol/l to 2.9 x 10(-4) mol/l. In both experimental situations a decrease of maximal reaction velocity (Vmax) was observed. At high concentration of potassium in incubation medium the ATPase of synaptosomes was significantly more sensitive to pentifylline than at low concentration of potassium. The inhibition of ATPase by pentifylline was not influenced by the change in Na+/K+ ratio in the incubation medium. In all these experiments, theophylline used as a standard xanthine, was virtually without effect on the reaction kinetic of Na+-, K+-ATPase.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008274 Magnesium A metallic element that has the atomic symbol Mg, atomic number 12, and atomic weight 24.31. It is important for the activity of many enzymes, especially those involved in OXIDATIVE PHOSPHORYLATION.
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D002395 Catecholamines A general class of ortho-dihydroxyphenylalkylamines derived from TYROSINE. Catecholamine,Sympathin,Sympathins
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D005260 Female Females
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
D000254 Sodium-Potassium-Exchanging ATPase An enzyme that catalyzes the active transport system of sodium and potassium ions across the cell wall. Sodium and potassium ions are closely coupled with membrane ATPase which undergoes phosphorylation and dephosphorylation, thereby providing energy for transport of these ions against concentration gradients. ATPase, Sodium, Potassium,Adenosinetriphosphatase, Sodium, Potassium,Na(+)-K(+)-Exchanging ATPase,Na(+)-K(+)-Transporting ATPase,Potassium Pump,Sodium Pump,Sodium, Potassium ATPase,Sodium, Potassium Adenosinetriphosphatase,Sodium-Potassium Pump,Adenosine Triphosphatase, Sodium, Potassium,Na(+) K(+)-Transporting ATPase,Sodium, Potassium Adenosine Triphosphatase,ATPase Sodium, Potassium,ATPase, Sodium-Potassium-Exchanging,Adenosinetriphosphatase Sodium, Potassium,Pump, Potassium,Pump, Sodium,Pump, Sodium-Potassium,Sodium Potassium Exchanging ATPase,Sodium Potassium Pump
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013574 Synaptosomes Pinched-off nerve endings and their contents of vesicles and cytoplasm together with the attached subsynaptic area of the membrane of the post-synaptic cell. They are largely artificial structures produced by fractionation after selective centrifugation of nervous tissue homogenates. Synaptosome

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