Vesicular monoamine transporter substrate/inhibitor activity of MPTP/MPP+ derivatives: a structure–activity study

…, BJ Heyen, IS Balasooriya, K Wimalasena

Index: Wimalasena, D. Shyamali; Perera, Rohan P.; Heyen, Bruce J.; Balasooriya, Inoka S.; Wimalasena, Kandatege Journal of Medicinal Chemistry, 2008 , vol. 51, # 4 p. 760 - 768

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Citation Number: 18

Abstract

The active metabolite of 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP), N-methyl-4- phenylpyridinium (MPP+), selectively destroys the dopaminergic neurons and induces the symptoms of Parkinson's disease. Inhibition of mitochondrial complex I and/or the perturbation of dopamine metabolism through cellular and granular accumulation have been proposed as some of the major causes of neurotoxicity. In the present study we have ...