Radiosynthesis of Sigma Receptor Ligands for Positron Emission Tomography: 11C- And 18F-labeled Guanidines

J Med Chem. 1991 Jun;34(6):1867-70. doi: 10.1021/jm00110a017.

Abstract

A series of analogues of the potent and selective sigma receptor ligand 1,3-ditolylguanidine (DTG) were synthesized and demonstrated to have high affinity for the sigma receptor as measured by in vitro [3H]DTG displacement studies using guinea pig brain tissue. Three of these 1-aryl-3-(1-adamantyl)guanidines were radiolabeled--two with carbon-11 and one with fluorine-18. Radiochemical yields and specific activities were sufficient for these radiotracers to be used in positron emission tomography imaging of the haloperidol-sensitive sigma receptor.

Publication types

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

MeSH terms

  • Animals
  • Carbon Radioisotopes*
  • Chromatography, High Pressure Liquid
  • Fluorine Radioisotopes*
  • Guanidines / chemical synthesis*
  • Guanidines / metabolism
  • Guinea Pigs
  • Magnetic Resonance Spectroscopy
  • Receptors, Opioid / metabolism*
  • Receptors, sigma
  • Tomography, Emission-Computed

Substances

  • Carbon Radioisotopes
  • Fluorine Radioisotopes
  • Guanidines
  • Receptors, Opioid
  • Receptors, sigma
  • 1,3-ditolylguanidine