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Relevance of benzyloxy group in 2‐indolyl methylamines in the selective MAO‐B inhibition
  • V. Pérez, J. L. Marco, Eldiberto Fernández‐Álvarez, Mercedes Unzeta
  • Chemistry, Medicine
  • British journal of pharmacology
  • 1 June 1999
A new series of molecules with structural features which determine the selectivity of MAO inhibition should provide a better understanding of the active site of monoamine oxidase and could be the starting point for the design of further selective, non‐amphetamine‐like MAO‐B inhibitors with therapeutic potential for the treatment of neurological disorders. Expand
Effect of the additional noradrenergic neurodegeneration to 6-OHDA-lesioned rats in levodopa-induced dyskinesias and in cognitive disturbances
The results suggest that levodopa-induced dyskinesias in the 6-OHDA-lesioned rats were not affected by the additional noradrenergic lesion, whereas this last condition was sufficient to worse the cognitive performance deficit produced by the dopaminergic lesions. Expand
FA-70, a novel selective and irreversible monoamine oxidase-A inhibitor: effect on monoamine metabolism in mouse cerebral cortex.
The ex vivo effect of FA70 on dopamine content was correlated with the activation effect on tyrosine hydroxylase activity, the enzyme responsible for the regulation of the limiting step in catecholamine synthesis. Expand
Molecular determinants of MAO selectivity in a series of indolylmethylamine derivatives: biological activities, 3D-QSAR/CoMFA analysis, and computational simulation of ligand recognition.
Comparing the steric and electrostatic properties at the 5 position of the indole ring are determinant for MAO selectivity and Computational simulations of the complex between this part of the ligand and Phe-208 or Ile-199 of MAO-B allowed us to further characterize the nature of these enzyme-inhibitor interactions. Expand
PF 9601N [N-(2-propynyl)-2-(5-benzyloxy-indolyl) methylamine], a new MAO-B inhibitor, attenuates MPTP-induced depletion of striatal dopamine levels in C57/BL6 mice
It can be concluded that PF 9601N attenuates MPTP neurotoxicity "in vivo" better than L-deprenyl through different mechanisms, with special relevance to the protective effect, independent of MAO-B inhibition, observed in the irreversibly MPTP-lesioned adult-old mice. Expand
The novel type B MAO inhibitor PF9601N enhances the duration of L-DOPA-induced contralateral turning in 6-hydroxydopamine lesioned rats
The results suggest that PF9601N may be used as a novel tool in the treatment of Parkinson's disease by enhancing the duration of contralateral rotational behavior with respect to L-DOPA plus vehicle in a dose-related manner. Expand
Sex-related effects of 1-methyl-4-phenyl-1,2,3,6-tetrahydro-pyridine treatment may be related to differences in monoamine oxidase B
Evidence is presented that MAO B may be involved in the sex related effects of MPTP, which depends on its conversion to the 1-methyl-4-phenylpyridinium ion (MPP+) by monoamine oxidase B (MAO B). Expand
Kinetic Studies of N‐Allenic Analogues of Tryptamine as Monoamine Oxidase Inhibitors
A series of N‐allenic analogues of tryptamine in which the side chain is located at the 2 position of the indole ring, but which differed in the ring and side‐chain nitrogen substituents, wereExpand
Kinetic behaviour of some acetylenic indolalkylamine derivatives and their corresponding parent amines.
Different methoxy indolalkylamines based on a common structure, and differing in the side chain attached at the 2 position of the indole ring were studied as MAO A inhibitors to establish the correlation with structural features that predetermine one compound to be a good MAO substrate or a goodMAO A and MAO B inhibitor. Expand
Protective effect of N‐(2‐propynyl)‐2‐(5‐benzyloxy‐indolyl) methylamine (PF 9601N), a novel MAO‐B inhibitor, on dopamine‐lesioned PC12 cultured cells
The results indicated that, besides the intracellular toxicity effect of dopamine, another non‐specific extracellular mechanism could be involved in the pathogenesis of Parkinson's disease. Expand