Positron emission tomography in drug evaluation: influence of three different catechol-O-methyltransferase inhibitors on metabolism of [NCA] 6-[18F]fluoro-L-dopa in rhesus monkey

Nucl Med Biol. 1995 Oct;22(7):921-7. doi: 10.1016/0969-8051(95)00032-s.

Abstract

We compared the influence of three different catechol-O-methyltransferase (COMT) inhibitors (CGP 28014, OR-611 and Ro 40-7592) on the metabolism of no-carrier-added (NCA) 6-[18F]fluoro-L-dopa (6-FDOPA) in one Rhesus monkey. All three COMT inhibitors improved 6-FDOPA availability in plasma, increased the specific uptake in the brain and thus improved 6-FDOPA uptake measurements using positron emission tomography (PET). Best results were obtained with Ro 40-7592.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amidines / pharmacokinetics
  • Amidines / pharmacology
  • Animals
  • Benzophenones / pharmacokinetics
  • Benzophenones / pharmacology
  • Biological Availability
  • Brain / drug effects
  • Brain / enzymology
  • Brain / metabolism
  • Catechol O-Methyltransferase Inhibitors*
  • Catechols / pharmacokinetics
  • Catechols / pharmacology
  • Dihydroxyphenylalanine / analogs & derivatives*
  • Dihydroxyphenylalanine / metabolism
  • Dihydroxyphenylalanine / pharmacokinetics
  • Drug Evaluation, Preclinical / methods
  • Enzyme Inhibitors / pharmacokinetics
  • Enzyme Inhibitors / pharmacology*
  • Female
  • Fluorine Radioisotopes
  • Macaca mulatta
  • Nitriles
  • Nitrophenols
  • Pyridones / pharmacokinetics
  • Pyridones / pharmacology
  • Tolcapone
  • Tomography, Emission-Computed

Substances

  • Amidines
  • Benzophenones
  • Catechol O-Methyltransferase Inhibitors
  • Catechols
  • Enzyme Inhibitors
  • Fluorine Radioisotopes
  • Nitriles
  • Nitrophenols
  • Pyridones
  • N-(2-pyridone-6-yl)-N',N'-di-n-propylformamidine
  • fluorodopa F 18
  • entacapone
  • Dihydroxyphenylalanine
  • Tolcapone