Interaction of pentobarbital with gabaergic drugs acting on the Cl(-)-ATPase activity of the plasma membranes from bream brain (Abramis brama L.).
The present study was designed to investigate the role of the interaction of pentobarbital with gamma-aminobutyric acid (GABA)ergic drugs acting on the Cl(-)-adenosine triphosphate (ATP)ase activity of the plasma membranes fraction of bream brain. The preincubation and then incubation of the membranes with pentobarbital as well as with other GABAergic ligands was conducted at physiologic pH (7.4), i.e. at the condition where the Cl(-)-ATPase activity is not detected. Pentobarbital (1-100 microM) induces Cl(-)-ATPase activity, however at high concentration (1,000 microM) no effect of the ligand was found. In addition pentobarbital (50 microM) enhances the effect of low concentration of GABA (1 microM) on the Cl(-)-ATPase activity, but inhibits the action of high concentration of GABA (100 microM) on the enzyme. Whereas no activating effect of pentobarbital in the presence of baclofen (1 microM) was found. The blocker of GABA(A)-receptors, picrotoxin (50 microM) and bicuculline (5 microM) eliminated the action of pentobarbital on the enzyme. The present results provide evidence for the first time that at physiologic pH in incubation medium the interaction of pentobarbital with GABAergic drugs on the Cl(-)-ATPase activity is similar to the effects of these ligands on the GABA(A)-receptor.
Menzikov
Sergey
S
Papanin Institute of Biology of Inland Waters, Russian Academy of Sciences, Borok, Yaroslavl Region, 152742 Russia. sam@ibiw.yaroslavl.ru
Menzikova
Olga
O
D000251:Adenosine Triphosphatases / Q000187:drug effects / Q000502:physiology*; D000818:Animals; D027321:Anion Transport Proteins; D001418:Baclofen / Q000494:pharmacology; D001640:Bicuculline / Q000494:pharmacology; D001921:Brain / Q000187:drug effects* / Q000201:enzymology; D002462:Cell Membrane / Q000187:drug effects* / Q000201:enzymology; D002712:Chlorides / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D018682:GABA Agents / Q000494:pharmacology*; D018756:GABA Antagonists / Q000494:pharmacology; D018757:GABA Modulators / Q000494:pharmacology*; D008297:Male; D010424:Pentobarbital / Q000494:pharmacology*; D010852:Picrotoxin / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects; D021541:Sea Bream; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology
D000251:Adenosine Triphosphatases; D027321:Anion Transport Proteins; D001418:Baclofen; D001640:Bicuculline; D002712:Chlorides; D018682:GABA Agents; D018756:GABA Antagonists; D018757:GABA Modulators; D010424:Pentobarbital; D010852:Picrotoxin; D011963:Receptors, GABA-A; D005680:gamma-Aminobutyric Acid; C031652:anion-sensitive ATPases