Quantification of methyllycaconitine, selective α7 nicotinic receptor antagonist, in rodent plasma and brain tissue by liquid chromatography tandem mass spectrometry--application to neuropharmacokinetics of methyllycaconitine in rats

Biomed Chromatogr. 2011 Nov;25(11):1273-82. doi: 10.1002/bmc.1603. Epub 2011 Feb 18.

Abstract

A sensitive high-performance liquid chromatography-positive ion electrospray tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantification of methyllycaconitine (MLA) in rat plasma and brain tissue. Following acetonitrile protein precipitation, the analyte was separated using a gradient mobile phase on a reversed-phase column and analyzed by MS/MS in the multiple reaction monitoring mode using the respective [M + H](+) ions, m/z 683-216 for MLA and m/z 260-116 for the internal standard. The assay exhibited a linear dynamic range of 0.5-250 ng/mL for MLA in rat plasma and brain tissue. The lower limit of quantification was 0.5 ng/mL. Acceptable precision (<12%) and accuracy (100 ± 6%) were obtained for concentrations over the standard curve range. The method was successfully applied to quantify MLA concentrations in a rodent pharmacokinetic and brain penetration study.

Keywords: brain tissue; liquid chromatography-tandem mass spectrometry; methyllycaconitine; pharmacokinetic study; plasma.

MeSH terms

  • Aconitine / analogs & derivatives*
  • Aconitine / analysis
  • Aconitine / blood
  • Aconitine / pharmacokinetics
  • Animals
  • Brain / metabolism
  • Brain Chemistry*
  • Chromatography, Liquid / methods*
  • Linear Models
  • Rats
  • Reproducibility of Results
  • Sensitivity and Specificity
  • Tandem Mass Spectrometry / methods*

Substances

  • methyllycaconitine
  • Aconitine