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

Marc Laruelle, Anissa Abi-Dargham, Zachary Rattner, Mohammed S. Al-Tikriti, Yolanda Zea-Ponce, Sami S. Zoghbi, Dennis S. Charney, Julie Price, J. James Frost, Paul B. Hoffer, Ronald M. Baldwin, Robert B. Innis

Research output: Contribution to journalArticle

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 permitted estimation of an equilibrium binding affinity constant of 0.47 nM and a maximum binding capacity of 127 nM in occipital cortex.

Original languageEnglish (US)
Pages (from-to)119-123
Number of pages5
JournalEuropean Journal of Pharmacology
Volume230
Issue number1
DOIs
StatePublished - Jan 5 1993

Keywords

  • Benzodiazepine receptors
  • SPECT (single photon emission tomography)
  • [I]Iomazenil

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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    Laruelle, M., Abi-Dargham, A., Rattner, Z., Al-Tikriti, M. S., Zea-Ponce, Y., Zoghbi, S. S., Charney, D. S., Price, J., Frost, J. J., Hoffer, P. B., Baldwin, R. M., & Innis, R. B. (1993). Single photon emission tomography measurement of benzodiazepine receptor number and affinity in primate brain: a constant infusion paradigm with [123I]iomazenil. European Journal of Pharmacology, 230(1), 119-123. https://doi.org/10.1016/0014-2999(93)90421-D