N-[11CH3]Dimethylaminoparthenolide (DMAPT) uptake into orthotopic 9LSF glioblastoma tumors in the rat

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5883-5886. doi: 10.1016/j.bmcl.2016.11.015. Epub 2016 Nov 9.

Abstract

The aim of this study was to determine the uptake of intravenously administered N-[11CH3]-dimethylaminoparthenolide (DMAPT) into orthotopic 9LSF glioblastoma brain tumors in Fisher 344 rats from positron emission tomography (PET) imaging studies. [11C]methyl iodide (11CH3I) was utilized as a [11C]-labeling reagent to label the precursor methylaminoparthenolide (MAPT) intermediate. From PET imaging studies it was found that brain uptake of N-[11CH3]DMAPT into brain tumor tissue was rapid (30min), and considerably higher than that in the normal brain tissue.

Keywords: Dimethylaminoparthenolide (DMAPT); PET-imaging; Uptake into brain; [(11)C]-labeled DMAPT.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Glioblastoma / diagnostic imaging*
  • Glioblastoma / pathology
  • Molecular Structure
  • Positron-Emission Tomography
  • Rats
  • Rats, Inbred F344
  • Sesquiterpenes / chemistry
  • Sesquiterpenes / pharmacokinetics*
  • Structure-Activity Relationship

Substances

  • LC-1 compound
  • Sesquiterpenes