[Effect of new 2-propinylamine derivatives on mitochondrial monoamine oxidase activity].
New derivatives of 2-propinyl amine were studied as possible inhibitors of mitochondrial monoamine oxidases (MAO) from rat liver and brain tissues. Kinetics of inhibition of the MAO activity (A and B types) is described for one of the substances studied -- N-(8-quinolyl methyl)-N-methyl-2-propinyl amine. Interaction of N-(8-quinolylmethyl)-N-methyl-2-propinyl amine with MAO of the A type (serotonin as a substrate) and of the B type (beta-phenylethylamine as a substrate) was studied by the kinetic method, which enabled to determine and quantitatively estimate the steps of enzyme-inhibitor complexes formation. The inhibition of the mitochondrial MAO A and B types by the substance was shown to include the steps of formation of dissociating enzyme-inhibitor intermediates with the subsequent irreversible modification of them. The data on K1 values, estimated in experiments with serotonin and beta-phenylethylamine as substrates, show that the affinity of N-(8-quinolyl methyl)-N-methyl-2-propinyl amine towards MAO of the A type was 10-fold higher than the affinity towards MAO of the B type. The rates of these complexes conversion into irreversibly blocked forms of the MAO A and B types was found to be similar.
D000480:Alkynes / Q000494:pharmacology; D000588:Amines / Q000494:pharmacology*; D000818:Animals; D001921:Brain / Q000201:enzymology; D004789:Enzyme Activation / Q000187:drug effects; D007700:Kinetics; D008928:Mitochondria / Q000187:drug effects* / Q000201:enzymology; D008930:Mitochondria, Liver / Q000187:drug effects* / Q000201:enzymology; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D010293:Pargyline / Q000031:analogs & derivatives; D010627:Phenethylamines / Q000494:pharmacology; D011437:Propylamines; D011804:Quinolines / Q000494:pharmacology; D051381:Rats; D012701:Serotonin / Q000494:pharmacology; D014439:Tyramine / Q000494:pharmacology
D000480:Alkynes; D000588:Amines; D008996:Monoamine Oxidase Inhibitors; D010627:Phenethylamines; D011437:Propylamines; D011804:Quinolines; C009054:propargylamine; D012701:Serotonin; D010293:Pargyline; D008995:Monoamine Oxidase; D014439:Tyramine
Vliianie novykh proizvodnykh 2-propinilamina na aktivnost' mitokhondrial'nykh monoaminoksidaz.