Quantification of amphetamine-induced changes in [11C]raclopride binding with continuous infusion

Richard E. Carson, Alan Breier, Andrea De Bartolomeis, Richard C. Saunders, Tom P. Su, Bernard Schmall, Margaret G. Der, David Pickar, William C. Eckelman

Research output: Contribution to journalArticlepeer-review

205 Scopus citations


Positron emission tomography and single-photon emission computer tomography receptor-binding ligands can be used to measure changes in neurotransmitter levels. In particular, amphetamine-induced dopamine release has been assessed with [11C]raclopride by paired bolus injections and with [123I]iodobenzamide by using a single bolus plus infusion (B/I) study. Here, we measured the change in [11C]raclopride-specific binding in rhesus monkeys after i.v. administration of 0.4 mg/kg amphetamine by using both the bolus and B/I paradigms. Paired bolus studies (control and postamphetamine) were analyzed using compartment modeling and graphical analysis with a new plasma metabolite model to measure the total distribution volume (V(T)). Specific binding, calculated with three measures linearly proportional to the binding potential, demonstrated a 22-42% reduction in the postamphetamine study. V(T) values from B/I studies were determined by the tissue-to-plasma ratio at equilibrium, in addition to the bolus methods. There was good agreement between the control V(T) values between bolus and B/I studies. The amphetamine-induced change in specific binding in B/I studies was 19 ± 16%, measured directly from tissue radioactivity levels. This study demonstrates that stimulus-induced changes in specific binding can be measured with a single [11C]raclopride study using the B/I method.

Original languageEnglish (US)
Pages (from-to)437-447
Number of pages11
JournalJournal of Cerebral Blood Flow and Metabolism
Issue number4
StatePublished - 1997
Externally publishedYes


  • Amphetamine
  • Infusion
  • Modeling
  • Raclopride

ASJC Scopus subject areas

  • Endocrinology
  • Neuroscience(all)
  • Endocrinology, Diabetes and Metabolism


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