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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 [ 11 C]raclopride by paired bolus injections and with [ 123 I]iodobenzamide by using a single bolus plus infusion (B/I) study. Here, we measured the change in [ 11 C]raclopride-specifìc 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 [ 11 C]raclopride study using the B/I method.

Quantification of Amphetamine-Induced Changes in [11C]Raclopride Binding with Continuous Infusion

Quantification of Amphetamine-Induced Changes in [¹¹C]Raclopride Binding with Continuous Infusion