In vivo quantification of dopamine D2 receptor parameters in nonhuman primates with [123I]iodobenzofuran and single photon emission computerized tomography

Eur J Pharmacol. 1994 Sep 22;263(1-2):39-51. doi: 10.1016/0014-2999(94)90521-5.

Abstract

[123I]Iodobenzofuran ([123I]IBF) is a new single photon emission computed tomography (SPECT) tracer for visualization of the dopamine D2 receptors. A tracer constant infusion paradigm was developed to measure the binding potential, density (Bmax) and affinity (KD) of the dopamine D2 receptor in baboons. Three baboons underwent both a single bolus and a constant infusion study. For the single bolus experiment, the striatal binding potential (134 +/- 24 ml g-1, mean +/- S.D.) was derived by kinetic analysis. For the constant infusion experiments, the striatal binding potential (127 +/- 16 ml g-1) was derived by equilibrium analysis. The two sets of experiments thus provided consistent data. Low specific activity constant infusion experiments were performed to measure KD (0.08 nM) and Bmax (12.7 nM). In vitro experiments carried out at 37 degrees C with [125I]IBF on rat striatal homogenate membranes provided results in agreement with the SPECT data. These studies suggested the feasibility of quantitation of dopamine D2 receptor parameters with [123I]IBF SPECT imaging.

Publication types

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

MeSH terms

  • Animals
  • Benzofurans
  • Binding Sites
  • Brain Chemistry*
  • Female
  • Iodine Radioisotopes
  • Kinetics
  • Male
  • Papio
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine D2 / analysis*
  • Receptors, Dopamine D2 / drug effects
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Benzofurans
  • Iodine Radioisotopes
  • Receptors, Dopamine D2