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Showing 1 to 20 of 22 for “"1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine"”.
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Studies on 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and analogs
The cyclic allylamine I-methyl-4-phenyl-l ,2,3,6-tetrahydropyridine (MPTP) is a potent and specific neurotoxin that causes a parkinsonian like syndrome in humans and subhuman primates. Research has revealed that MPTP is bioactivated in a reaction catalyzed by flavin containing monoamine oxidase B …
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Quantitative structure activity relationships of monoamine oxidase catalyzed oxidation of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine analogs
… structure act! Vlty relationships of rate s of I-methyl-4-phenyl-l,2,3,6-tetrahydropyridine oxidation catalyzed by monoamine oxidases A and B were performed to elucidate active site substrate conformation and oxidation mechanisms. Plotting experimental kinetic activity against molecular properties …
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Effects of Central and Peripheral Administration of 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine (Mptp) in the Rat and Mouse
… cells and converted to its neurotoxic form N-methyl-4-phenyl pyridinium ion (MPP+), and 2), this is followed by uptake of MPP+ by dopaminergic cells via an uptake system. The above two steps are necessary for the neurotoxicity of MPTP to be exhibited. To determine whether direct intranigral …
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Potential Prodrugs of the Neuronal Nitric Oxide Synthase and Monoamine Oxidase Inhibitor 7-Nitroindazole and Structurally Related Compounds
… employs the parkinsonian inducing neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). One such compound is 7-nitroindazole (7-NI), a compound which is reported to inhibit both enzymes. This thesis focuses on the synthesis and biological evaluation of a potential prodrug form of 7-NI …
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Synthesis and mechanistic studies on the monoamine oxidase (MAO) catalyzed oxidation of 1,4-disubstituted-1,2,3,6-tetrahydropyridines
The parkinsonian inducing drug 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) is bioactivated in a reaction catalyzed by the flavoenzyme monoamine oxidase B (MAO-B) to form the corresponding dihydropyridinium (MPDP+) subsequently pyridinium (MPP+) metabolites. As part of our ongoing studies to …
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Vulnerability to cognitive, neurotoxic and neuroinflammatory effects of toxins that induce Parkinson's disease after administration of amphetamine-related drugs in mice
… disease (PD) in amphetamine users. 3,4-Methylenedioxymethamphetamine (MDMA) is an amphetamine-related drug which may have neuroinflammatory and neurotoxic effects. The present study was aimed at evaluating in mice whether administration of MDMA during adolescence might influence …
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Study on the Neuroprotective Effects of Ethyl pyurvate in MPTP-induced Mouse PD Models
… nigrostriatal dopaminergic (DA) neurons in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model of Parkinson’s disease. MPTP induced degeneration of nigrostriatal DA neurons and glial activation as visualized by tyrosine hydroxylase, macrophage antigen complex-1, and/or glial …
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Investigation of FAD Chemical Models to Study the Monoamine Oxidase Catalyzed Oxidation of Cyclic Tertiary-Allylamines
… oxidation of the cyclic tertiary allylamine 1-methyl-4-(2-methyl-1H-pyrrol-2-yl)-1,2,3,6-tetrahydropyridine (TMMP), which is a close analog of the parkinsonian-inducing designer drug 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). MAO-B catalyzes the conversion of MPTP and its derivatives …
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Oxidation of Tetrahydropyridines by MAO B Biomimetics: Mechanistic Studies
The Parkinsonian Syndrome-inducing effects of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) on the body have been well-documented since its discovery. However, its mechanism of oxidation by monoamine oxidase B (MAO B) has been debated for just as long. Proponents of the single electron …
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A study of the neurotoxicity of MPTP and analogs in human neuroblastoma SH-SY5Y cells
… from exposure to Parkinsonian-inducing 1-methyl-4- phenyl-1,2,3,6-tetrahydropyridine (MPTP) in an in vitro model SH-SYSY human neuroblastoma cells were explored using cytotoxic effects, neurochemical changes and pathological injury as endpoints. The results suggested that: MPTP entered the …
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Metabolic Studies on 1-Cyclopropyl-4-phenyl-1,2,3,6-tetrahydropyridinyl Derivatives by HPLC and LC-ESI/MS
… of the parkinsonian inducing agent 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) to generate the neurotoxic 1-methyl-4-phenylpyridinium species (MPP+) is well documented. The N-cyclopropyl analog (CPTP) of MPTP is a mechanism based inactivator of MAO-B which presumably is …
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Glutamate Imaging of Mouse Models of Neurodegeneration
… transgenic model of tau pathology, and the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) neurotoxin model of PD. Glutamate levels derived from GluCEST imaging were correlated with results from 1HMRS and immunohistochemistry (IHC). The primary IHC antibodies that were investigated include …
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Effects of MPTP, MPP(+) and Adreno-Medullin on Dopamine Metabolism in the Rat Corpus Striatum
Self-administration of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), a contaminant on illicit narcotic drugs, causes parkinsonism symptoms in drug addicts. Also, systemic injections of very low doses of MPTP in non-human primates produces selective destruction of the nigrostriatal dopamine …
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Mechanistic Studies on the Monoamine Oxidase B Catalyzed Oxidation of 1,4-Disubstituted Tetrahydropyridine Derivatives
… and inactivator properties of 1,4-disubstituted tetrahydropyridine derivatives to probe the mechanism of MAO-B catalysis. Reports of the parkinsonian inducing neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) as a structurally unique substrate of MAO-B initiated these studies. …
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The Investigation of the Active Sites of Monoamine Oxidase (MAO) A and B and the Study of MAO-A Mediated Neurotoxicity Using 4-Substituted Tetrahydropyridines
… properties of various 1,4-disubstituted-1,2,3,6-tetrahydropyridine derivatives offer an interesting opportunity to probe the active sites of MAO-A and MAO-B. In an effort to explore the spatial features of the active sites, we have synthesized series of substituted tetrahydropyridines, evaluated …
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Studies on the metabolic bioactivation of haloperidol (HP) and its tetrahydropyridine dehydration product
… to a drug-induced neuronal lesion. HP and its tetrahydropyridine dehydration product {4-(4-chlorophenyl)-1- [4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydropyridine (HPTP) share structural features with the parkinsonian inducing neurotoxin 1-Methyl-4- phenyl-1,2,3,6-tetrahydropyridine (MPTP). …
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Insecticide-Mediated Neurochemical and Behavioral Changes as Possible Predisposing Environmental Factors in Idiopathic Parkinson's Disease
… by the established parkinsonian neurotoxicant, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). At the end of the treatment period, mice were assessed for effects on behavior, as well as levels of striatal dopamine, nerve terminal respiration, and synaptosomal dopamine transport. The primary …
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Neuronal and Mitochondrial Protection in Chronic Parkinsonism
… The aged chronic MPD was treated with of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) (15 mg/kg, s.c), twice a week for 5 weeks. MPTP was co-administered with probenecid (250 mg/kg, i.p), an adjuvant that is known to inhibit the peripheral and neuronal clearance of MPTP and potentiate …
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Synthesis and biological evaluation of novel MPTP analogs as potential monoamine oxidase B inhibitors
The Parkinsonian-inducing neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and close structural analogs are the only known cyclic tertiary amines with good monoamine oxidase substrate properties. In addition to its substrate properties, MPTP is a weak mechanism-based inactivator of …
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Proteomic analysis of cellular models of neurodegeneration and mitochondrial dysfunction
… observed in Parkinson’s disease patients and 1-methyl-4-phenyl-1,2,3,6 tetrahydropyridine (MPTP), a complex I inhibitor, produces a Parkinsonian state in mammals. The aims of the present study were to determine the effects of MPTP on the mitochondrial proteome in a cellular model using mouse N2a …
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