Neuroprotective potential of Linezolid: a quantitative and distribution study via mass spectrometry

J Mol Histol. 2016 Aug;47(4):429-35. doi: 10.1007/s10735-016-9685-0. Epub 2016 Jun 21.


A study was undertaken to determine the neuroprotective potential of Linezolid (LIN) in an animal model. Female Sprague-Dawley rats were either given a single (100 mg/kg) dose or treated daily for 4 weeks. A validated LC-MS/MS method was used to measure LIN levels in plasma and brain, this was paired with mass spectrometry imaging to determine the tissue spatial distribution of the drug. The results showed that after a single dose there was poor penetration of the drug into the brain. With multiple doses there were high tissue levels, with the drug reaching steady state in subsequent weeks. LIN displayed a promising distribution pattern with localisation in the brainstem. Systemic circulation is fed into the brain by the carotid and vertebral arteries which enter through the brain stem, therefore high drug concentrations is this area may protect against infectious agents entering via this route.

Keywords: Brain; LC–MS/MS; Linezolid; MSI; Molecular histology; Neuroprotection.

MeSH terms

  • Animals
  • Brain / metabolism
  • Chromatography, Liquid
  • Female
  • Linezolid / pharmacokinetics*
  • Mass Spectrometry / methods
  • Neuroprotective Agents / pharmacokinetics*
  • Rats
  • Tandem Mass Spectrometry
  • Tissue Distribution


  • Neuroprotective Agents
  • Linezolid