Brain Regional Pharmacokinetics of p-Aminosalicylic Acid and Its N-Acetylated Metabolite: Effectiveness in Chelating Brain Manganese

@article{Hong2011BrainRP,
  title={Brain Regional Pharmacokinetics of p-Aminosalicylic Acid and Its N-Acetylated Metabolite: Effectiveness in Chelating Brain Manganese},
  author={Lan Young Hong and Wendy Jiang and Hao Pan and Yueming Jiang and Su Zeng and Wei Zheng},
  journal={Drug Metabolism and Disposition},
  year={2011},
  volume={39},
  pages={1904 - 1909}
}
para-Aminosalicylic acid (PAS; 4-amino-2-hydroxybenzoic acid), an antituberculosis drug in use since the 1950s, has recently been suggested to be an effective agent for treatment of manganese-induced parkinsonian disorders. However, the neuropharmacokinetics of PAS and its metabolite N-acetyl-para-aminosalicylic acid (AcPAS; N-acetyl-4-amino-2-hydroxybenzoic acid) are unknown. This study was designed to investigate the pharmacokinetics of PAS and its distribution in brain to help better design… Expand
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TLDR
The method was used to quantify PAS and AcPAS in rat plasma and brain following a single iv injection of P AS and showed a greater amount of PAS than AcP AS in plasma, while a greater amounts of AcPas than PAS was found in brain tissues. Expand
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TLDR
Data suggest that PAS likely acts as a chelating agent to mobilize and remove tissue Mn, and a high-dose and prolonged PAS treatment appears necessary for its therapeutic effectiveness. Expand
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Under the Pb exposure and chelation treatment regimens utilized here, there was no evidence of a measurable redistribution of endogenous Pb into the brain after a single CaNa(2)EDTA dose, and CaNa (2) EDTA was not efficacious in measurably reducing brain or bone Pb levels, although brain levels of labile (204)Pb tracer were significantly reduced after 5 days of chelation. Expand
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TLDR
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TLDR
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