Specific binding of 3N-(2'-[18F]fluoroethyl)benperidol to primate cerebral dopaminergic D2 receptors demonstrated in vivo by PET

Neurosci Lett. 1992 Dec 14;148(1-2):97-100. doi: 10.1016/0304-3940(92)90813-m.

Abstract

3N-(2'-[18F]Fluoroethyl)benperidol ([18F]FEB) an 18F-labeled analogue of the D2 antagonist benperidol, was evaluated as a tracer for positron emission tomography (PET). PET imaging of a living baboon showed that the fluorinated ligand rapidly localized in vivo within D2 receptor-rich brain tissue, with selective retention lasting over 2 h after tracer injection. Pretreatment of the animal with unlabeled D2-specific antagonist eticlopride (4 mg/kg, i.v.) 1 h before [18F]FEB completely abolished the selective disposition of the radioligand, whereas the regional cerebral blood flow, blood volume and peripheral metabolism/protein binding of [18F]FEB were not changed. Tracer localization when the baboon was pretreated with unlabeled ketanserin (0.55 mg/kg, i.v.) or SCH 23390 (1.1 mg/kg, i.v.) was identical to that for the control case, indicating that the [18F]FEB did not bind to S2 of D1 receptors in vivo. [18F]FEB has advantages compared to previously used PET tracers, and may be an excellent radioligand for non-invasive study of D2 receptor binding.

Publication types

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

MeSH terms

  • Animals
  • Basal Ganglia / diagnostic imaging
  • Basal Ganglia / drug effects
  • Basal Ganglia / metabolism
  • Benperidol / analogs & derivatives*
  • Benperidol / metabolism
  • Benzazepines / pharmacology
  • Brain / diagnostic imaging
  • Brain / metabolism*
  • Cerebellum / diagnostic imaging
  • Cerebellum / metabolism
  • Dopamine D2 Receptor Antagonists
  • Fluorine Radioisotopes
  • Ketanserin / pharmacology
  • Kinetics
  • Papio
  • Receptors, Dopamine D2 / drug effects
  • Receptors, Dopamine D2 / metabolism*
  • Salicylamides / pharmacology
  • Tomography, Emission-Computed / methods

Substances

  • Benzazepines
  • Dopamine D2 Receptor Antagonists
  • Fluorine Radioisotopes
  • Receptors, Dopamine D2
  • Salicylamides
  • 3N-(2'-fluoroethyl)benperidol
  • Ketanserin
  • Benperidol
  • eticlopride