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Showing 1 to 20 of 32 for “"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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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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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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Quantitative structure activity relationships of monoamine oxidase catalyzed oxidation of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine analogs
… 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 obtained by experiment …
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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
MPTP has been observed to cause irreversible symptoms of parkinsonism associated with selective degeneration of the substantia nigral dopamine neurons in the midbrain of man and monkeys. Although rodents are less sensitive to the neurotoxic action of MPTP, it has been found that central …
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Synthetic and metabolic studies on 1-methyl-4-(1-methylpyrrol-2-yl)-1,2,3,6-tetrahydropyridine, a neurotoxic analog of the Parkinsonian inducing agent MPTP
1-Methyl-4-(1-methylpyrrol-2-yl)-1 ,2,3,6-tetrahydropyridine (TMMP) is a neurotoxic analog of the parkinsonian inducing agent MPTP. TMMP and its putative metabolites 1-methyl-4-(1-methylpyrrol-2-yl)-2,3-dihydropyridinium (MMDP+) and 1-methyl-4-(1-methylpyrrol-2-yl)pyridinium (MMP+) were synthesized …
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Synthesis and biological evaluation of novel MPTP analogs as potential monoamine oxidase B inhibitors
… 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 monoamine …
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Beitrag zur Chemie der 2,3,4,5-Tetrahydropyridine: Synthese von cyclischen Beta-Aminosäuren, Beta-Lactamen und Beta-Peptiden sowie schwefelhaltigen Gamma- und Delta-Lactamen und Alpha-Aminophosphonsäurederivaten
… substituierter und funktionalisierter 2,3,4,5-Tetrahydropyridine beschrieben. Der entscheidende Reaktionsschritt beschreibt die zweifache Addition von Organocerverbindungen an ein Nitril. Die cyclischen Imine werden in den folgenden Kapiteln für verschiedene Additionsreaktionen eingesetzt. …
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Synthetic and metabolic studies on centrally acting amines
… was converted to 1-(phenylcyclohexyl)- 1,2,3,4-tetrahydropyridine-5-carboxaldehyde. The same product was identified in the corresponding liver mitochondrial and microsomal incubation mixtures and in liver microsomal incubations of phencyclidine. The chemical conversion of the synthetic tetra …
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Investigation of FAD Chemical Models to Study the Monoamine Oxidase Catalyzed Oxidation of Cyclic Tertiary-Allylamines
… 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 into active neurotoxins in the brain that …
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Scope and stereochemistry of carbon-carbon bond formation via addition of carbon nucleophiles to nitrones
… in the reactions of cis-3,5-dimethyl-2,3,4,5-tetrahydropyridine N-oxide with both methyl and phenyl Grignard reagents and the silyl ketene acetal of t-butyl acetate. However, similar additions of carbon nucleophiles to 4-t-butyl-2,3,4,5-tetrahydropyridine N-oxide afforded only the trans isomer …
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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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Development of New N-Cyclopropyl Based Electron Transfer Probes for Cytochrome P-450 and Monoamine Oxidase Catalyzed Reactions
… the MAO-B substrate 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and two of its derivatives, 1-cyclopropyl-4-phenyl-1,2,3,6-tetrahydropyridine and (+/-)-[trans-2-phenylcyclopropyl-4-phenyl-1,2,3,6-tetrahydropyridine is presented in Chapter 2. The barrier for ring opening of aminyl …
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Synthesis and Characterization of 1-Methyl-4-Substituted-3-Piperidine-Carboxylic Acid N, N-Diethyamide.
… the brain, it was found that 1-methyl-1,2,5, 6-tetrahydropyridine-3-(N,N-diethylcarboxamide) (THPC), a compound similar in structure to the D-ring of LSD (Figure 1), blocked the behavioral disruption in rats induced by LSD as measured by Bovet-Gatti profiles on a Sidman avoidance schedule. …
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Potential Prodrugs of the Neuronal Nitric Oxide Synthase and Monoamine Oxidase Inhibitor 7-Nitroindazole and Structurally Related Compounds
… 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 and related indazolyl …
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Synthesis and mechanistic studies on the monoamine oxidase (MAO) catalyzed oxidation of 1,4-disubstituted-1,2,3,6-tetrahydropyridines
… 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
… effects of 1-methyl-4- phenyl-1,2,3,6-tetrahydropyridine (MPTP), a toxin known to induce PD in humans, in motor, limbic and cortical areas, and consequently affects cognitive performance. Mice received MDMA (10 mg/kg, twice a day/a week) for 9 weeks, followed by MPTP (20 mg/kg × 4 …
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Study on the Neuroprotective Effects of Ethyl pyurvate in MPTP-induced Mouse PD Models
… (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 fibrillary acidic protein …
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The synthesis and pharmacology of gamma-aminobutyric acid receptor mimetics
… Recently, it has been suggested that 1,2,3,6 Tetrahydropyridine-4-carboxylic acid (Isoguvacine) is a potent GABA receptor agonist. It has also been reported to act as a mixed agonist/antagonist at the GABA-benzodiazepine receptor complex. The binding of 3H-Isoguvacine to frozen-thawed, rat …
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Oxidation of Tetrahydropyridines by MAO B Biomimetics: Mechanistic Studies
… 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 transfer (SET) pathway of …
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