Single photon emission tomography measurement of benzodiazepine receptor number and affinity in primate brain: a constant infusion paradigm with [123I]iomazenil

Eur J Pharmacol. 1993 Jan 5;230(1):119-23. doi: 10.1016/0014-2999(93)90421-d.

Abstract

Benzodiazepine receptor number and affinity were measured in vivo with single photon emission tomography (SPECT). Following an initial bolus injection, the radiotracer [123I]iomazenil was infused at a constant rate for 5 to 8 h. This procedure induced a state of sustained equilibrium at the receptor level. Nondisplaceable activity was measured after injection of a receptor saturating dose of flumazenil. Experiments performed at high and low specific activity permitted estimation of an equilibrium binding affinity constant of 0.47 nM and a maximum binding capacity of 127 nM in occipital cortex.

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 Chemistry / drug effects*
  • Flumazenil / analogs & derivatives*
  • In Vitro Techniques
  • Iodine Radioisotopes
  • Papio
  • Receptors, GABA-A / drug effects*
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Iodine Radioisotopes
  • Receptors, GABA-A
  • Flumazenil
  • iomazenil