Carbon-11 labeled radioligands for imaging brain cannabinoid receptors

Nucl Med Biol. 2002 Aug;29(6):671-7. doi: 10.1016/s0969-8051(02)00308-6.

Abstract

Two radioligands, [(11)C] SR149080 and its morpholino analog [(11)C] SR149568, were synthesized by reaction of the respective phenolic precursors with [(11)C] methyl iodide. Both radioligands had appropriate regional brain distribution for cannabinoid receptors in mice with peak target to non-target ratios of 2.2 for [(11)C] SR149080 and 1.6 for [(11)C] SR149568 at 90 and 30 minutes post-injection respectively. The uptake of both tracers was blocked with a 1 mg/kg dose of SR141716A.

Publication types

  • Comparative Study
  • Evaluation Study

MeSH terms

  • Animals
  • Brain / diagnostic imaging*
  • Brain / metabolism*
  • Carbon Radioisotopes / pharmacokinetics*
  • Male
  • Mice
  • Morpholines / chemical synthesis
  • Morpholines / pharmacokinetics*
  • Piperidines / chemical synthesis
  • Piperidines / pharmacokinetics*
  • Pyrazoles / chemical synthesis
  • Pyrazoles / pharmacokinetics*
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics
  • Receptors, Cannabinoid
  • Receptors, Drug / metabolism*
  • Sensitivity and Specificity

Substances

  • Carbon Radioisotopes
  • Morpholines
  • N-(piperidin-1-yl)-5-(4-methoxyphenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
  • Piperidines
  • Pyrazoles
  • Radiopharmaceuticals
  • Receptors, Cannabinoid
  • Receptors, Drug
  • SR 149568