2Beta-carbomethoxy-3beta-(4- and 2-[18F]fluoromethylphenyl)tropanes: specific probes for in vivo quantification of central dopamine transporter sites

Nucl Med Biol. 1999 Nov;26(8):897-903. doi: 10.1016/s0969-8051(99)00073-6.

Abstract

Dopamine reuptake transporter binding kinetics of 2beta-carbomethoxy-3beta-(4-[18F]fluoromethylphenyl)tropane (p-FWIN) and 2beta-carbomethoxy-3beta-(2-[18F]fluoromethylphenyl)tropane (o-FWIN) were determined in vervet monkeys using positron emission tomography (PET). Ligand localization was rapid and specific to the striatum with kinetic estimates comparable with those of 11C-labeled WIN 35,428 (CWIN). Binding was more specific with p-FWIN than with CWIN or o-FWIN. The relatively longer half-life of the 18F radiolabel enabled longer acquisition times with p-FWIN, resulting in less variability in the kinetic estimates.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Brain / diagnostic imaging
  • Brain Chemistry*
  • Carrier Proteins / metabolism*
  • Chlorocebus aethiops
  • Cocaine / analogs & derivatives
  • Cocaine / pharmacokinetics
  • Dopamine Plasma Membrane Transport Proteins
  • Dopamine Uptake Inhibitors / pharmacokinetics
  • Image Processing, Computer-Assisted
  • Ligands
  • Membrane Glycoproteins*
  • Membrane Transport Proteins*
  • Nerve Tissue Proteins*
  • Norepinephrine / metabolism
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacokinetics
  • Radiopharmaceuticals / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine / metabolism*
  • Serotonin / metabolism
  • Tomography, Emission-Computed
  • Tropanes / chemical synthesis*
  • Tropanes / pharmacokinetics
  • Tropanes / pharmacology

Substances

  • 2-carbomethoxy-3-(2-fluoromethylphenyl)tropane
  • 2-carbomethoxy-3-(4-fluoromethylphenyl)tropane
  • Carrier Proteins
  • Dopamine Plasma Membrane Transport Proteins
  • Dopamine Uptake Inhibitors
  • Ligands
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • Radiopharmaceuticals
  • Receptors, Dopamine
  • Tropanes
  • Serotonin
  • (1R-(exo,exo))-3-(4-fluorophenyl)-8-methyl-8- azabicyclo(3.2.1)octane-2-carboxylic acid, methyl ester
  • Cocaine
  • Norepinephrine