1-Methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine metabolism and monoamine oxidase-B activity in rat brain

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Correlation of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine neurotoxicity with blood-brain barrier monoamine oxidase activity.

Systemic administration of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) causes parkinsonism in humans and subhuman primates, but not in rats and many other laboratory animals; mice are intermediate in their susceptibility. Since MPTP causes selective dopaminergic neurotoxicity when infused directly into rat substantia nigra, we hypothesized that systemic MPTP may be metabolized by monoam...

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Oxidation and enzyme-activated irreversible inhibition of rat liver monoamine oxidase-B by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP).

The compound 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), which produces symptoms resembling Parkinson's disease in humans, acts both as a substrate and an enzyme-activated irreversible inhibitor of the B-form of monoamine oxidase from rat liver. Analysis of the inhibitory process showed the compound to be considerably more efficient as a substrate than as an irreversible inhibitor, wit...

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Deuterium isotope effect measurements on the interactions of the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine with monoamine oxidase B.

Kinetic deuterium isotope effects for the noncompetitive, intermolecular monoamine oxidase B-catalyzed oxidation of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) to the corresponding 1-methyl-4-phenyl-2,3-dihydropyridinium species MPDP+ were found to be 3.55 on Vmax and 8.01 on Vmax/Km with MPTP-6,6-d2 as the deuterated substrate. Similar values were obtained with MPTP-2,2,6-d4 and MPTP-C...

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Neuro-rescue role of epicatechin-3-gallate on 1-methyl-4-phenyl- 1, 2, 3, 6 -tetrahydropyridine induced parkinsonic mice

Green tea polyphenols are known to possess various neuropharmacological properties. In the recent past, mice models using 1-methyl-4-phenyl-1, 2, 3, 6tetrahydropyridine (MPTP) have been widely used to study underlying mechanism of Parkinson’s disease. In this study, we examined the neurorescue properties of Epicatechin-3-gallate (ECG) against MPTP induced oxidative damage, neurotoxicity and beh...

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Synthesis and Antimicrobial Activity of Some 2-[(4-Substituted-Phenyl-3-Chloro-Azetidin-2-One)-5-(2'-Methylamino-4-Phenyl-1', 3'-Thiazolyl-]-1, 3,4-Thiadiazoles

A new 2-[(4-substituted-phenyl-3-chloroazetidin-2-one)-5-(2'-methylamino 4-phenyl-1', 3'-thiazolyl-]-1, 3, 4-thiadiazoles, 5(a-n) were synthesized from 2-substituted-benzylideneamino-5-[2'-methylamino-4'-phenyl-1',3'-thiazolyl]-1,3, 4-thiadiazole, 4(a-n) using 2-amino-4phenyl-1, 3-thiazole as a starting material. The synthesised compounds have been screened in vitro for their antimicrobial acti...

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ژورنال

عنوان ژورنال: Japanese Journal of Pharmacology

سال: 1986

ISSN: 0021-5198

DOI: 10.1016/s0021-5198(19)58954-5