Biomaterial Database

[Effect of new 2-propinylamine derivatives on mitochondrial monoamine oxidase activity]. 1977

K K Shatemirova, and G A Davydova, and I V Verevkina, and A I Tichilkin

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.

UI	MeSH Term	Description	Entries
D007700	Kinetics	The rate dynamics in chemical or physical systems.
D008928	Mitochondria	Semiautonomous, self-reproducing organelles that occur in the cytoplasm of all cells of most, but not all, eukaryotes. Each mitochondrion is surrounded by a double limiting membrane. The inner membrane is highly invaginated, and its projections are called cristae. Mitochondria are the sites of the reactions of oxidative phosphorylation, which result in the formation of ATP. They contain distinctive RIBOSOMES, transfer RNAs (RNA, TRANSFER); AMINO ACYL T RNA SYNTHETASES; and elongation and termination factors. Mitochondria depend upon genes within the nucleus of the cells in which they reside for many essential messenger RNAs (RNA, MESSENGER). Mitochondria are believed to have arisen from aerobic bacteria that established a symbiotic relationship with primitive protoeukaryotes. (King & Stansfield, A Dictionary of Genetics, 4th ed)	Mitochondrial Contraction,Mitochondrion,Contraction, Mitochondrial,Contractions, Mitochondrial,Mitochondrial Contractions
D008930	Mitochondria, Liver	Mitochondria in hepatocytes. As in all mitochondria, there are an outer membrane and an inner membrane, together creating two separate mitochondrial compartments: the internal matrix space and a much narrower intermembrane space. In the liver mitochondrion, an estimated 67% of the total mitochondrial proteins is located in the matrix. (From Alberts et al., Molecular Biology of the Cell, 2d ed, p343-4)	Liver Mitochondria,Liver Mitochondrion,Mitochondrion, Liver
D008995	Monoamine Oxidase	An enzyme that catalyzes the oxidative deamination of naturally occurring monoamines. It is a flavin-containing enzyme that is localized in mitochondrial membranes, whether in nerve terminals, the liver, or other organs. Monoamine oxidase is important in regulating the metabolic degradation of catecholamines and serotonin in neural or target tissues. Hepatic monoamine oxidase has a crucial defensive role in inactivating circulating monoamines or those, such as tyramine, that originate in the gut and are absorbed into the portal circulation. (From Goodman and Gilman's, The Pharmacological Basis of Therapeutics, 8th ed, p415) EC 1.4.3.4.	Amine Oxidase (Flavin-Containing),MAO,MAO-A,MAO-B,Monoamine Oxidase A,Monoamine Oxidase B,Type A Monoamine Oxidase,Type B Monoamine Oxidase,Tyramine Oxidase,MAO A,MAO B,Oxidase, Monoamine,Oxidase, Tyramine
D008996	Monoamine Oxidase Inhibitors	A chemically heterogeneous group of drugs that have in common the ability to block oxidative deamination of naturally occurring monoamines. (From Gilman, et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p414)	MAO Inhibitor,MAO Inhibitors,Reversible Inhibitors of Monoamine Oxidase,Monoamine Oxidase Inhibitor,RIMA (Reversible Inhibitor of Monoamine Oxidase A),Reversible Inhibitor of Monoamine Oxidase,Inhibitor, MAO,Inhibitor, Monoamine Oxidase,Inhibitors, MAO,Inhibitors, Monoamine Oxidase
D010293	Pargyline	A monoamine oxidase inhibitor with antihypertensive properties.	Pargyline Hydrochloride,Hydrochloride, Pargyline
D010627	Phenethylamines	A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)	Phenylethylamines
D011437	Propylamines	Derivatives of propylamine (the structural formula NH2CH2CH2CH3).
D011804	Quinolines
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