Potent neurotoxic fluorinated 1‐methyl‐4‐phenyl‐1,2,3,6‐tetrahydropyridine analogs as potential probes in models of parkinson disease

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dc.contributor.author Riachi, Naji J.
dc.contributor.author Arora, Pramod K.
dc.contributor.author Sayre, Lawrence M.
dc.contributor.author Harik, Sami I.
dc.date.accessioned 2019-04-15T10:27:33Z
dc.date.available 2019-04-15T10:27:33Z
dc.date.copyright 1988 en_US
dc.date.issued 2019-04-15
dc.identifier.issn 1471-4159 en_US
dc.identifier.uri http://hdl.handle.net/10725/10435
dc.description.abstract We synthesized a number of fluorinated analogs of 1‐methyl‐4‐phenyl‐1,2,3,6‐tetrahydropyridine (MPTP), and tested their suitability as substrates for monoamine oxidase B in vitro and their dopaminergic neurotoxicity in vivo. Two of the compounds tested, 2′‐F‐MPTP and 2′‐CF3‐MPTP, were better enzyme substrates and possessed more potent neurotoxicity for nigrostriatal dopamine neurons than MPTP, especially 2′‐F‐MPTP. The results of the in vivo neurotoxicity experiments correlated well with the suitability of the compounds as substrates for monoamine oxidase. These findings could serve as a basis for the use of 18F‐labeled analogs of MPTP for positron emission tomography studies of nonhuman primates for better understanding of the factors underlying MPTP toxicity. Furthermore, the discovery of two MPTP analogs with enhanced selective neurotoxicity to dopaminergic neurons may be an important clue in the continuing efforts to define the chemical structure‐activity factors governing MPTP neurotoxic activation mechanisms. en_US
dc.language.iso en en_US
dc.title Potent neurotoxic fluorinated 1‐methyl‐4‐phenyl‐1,2,3,6‐tetrahydropyridine analogs as potential probes in models of parkinson disease en_US
dc.type Article en_US
dc.description.version Published en_US
dc.author.school SOM en_US
dc.author.idnumber 200902731 en_US
dc.author.department N/A en_US
dc.description.embargo N/A en_US
dc.relation.journal Journal of Neurochemistry en_US
dc.journal.volume 50 en_US
dc.journal.issue 4 en_US
dc.article.pages 1319-1321 en_US
dc.keywords Fluorinated 1‐methyl‐4‐phenyl‐1,2,3,6‐tetrahydropyridine analogs en_US
dc.keywords Monoamine oxidase en_US
dc.keywords Neurotoxicity en_US
dc.identifier.doi https://doi.org/10.1111/j.1471-4159.1988.tb10610.x en_US
dc.identifier.ctation Riachi, N. J., Arora, P. K., Sayre, L. M., & Harik, S. I. (1988). Potent Neurotoxic Fluorinated 1‐Methyl‐4‐Phenyl‐1, 2, 3, 6‐Tetrahydropyridine Analogs as Potential Probes in Models of Parkinson Disease. Journal of neurochemistry, 50(4), 1319-1321. en_US
dc.author.email naji.riachi@lau.edu.lb en_US
dc.identifier.tou http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php en_US
dc.identifier.url https://onlinelibrary.wiley.com/doi/abs/10.1111/j.1471-4159.1988.tb10610.x en_US
dc.orcid.id https://orcid.org/0000-0002-8652-9698 en_US
dc.author.affiliation Lebanese American University en_US

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