In vivo characteristics of IBZM in rat brains: An agent for quantitative SPECT imaging of D₂ dopamine receptors - A basis for semiquantitative measurement of the receptor density using equilibrium analysis

To establish a basis for semiquantitative SPECT measurements of the D₂ dopamine receptor density using equilibrium analysis, we evaluated in vivo kinetic properties of ¹²⁵I-IBZM in rat brains. We measured percent uptakes (% dose/g) of ¹²⁵I-IBZM in the striatum, frontal cortex, and cerebellum. We made these regional measurements at 15, 30, 45, 60, 90, and 120 minutes after injection, respectively. The specific striatal uptake, which is the uptake difference between striatum and frontal cortex or cerebellum, showed a transient equilibrium phase at 60 min. Theoretically, with these 'reversible' D₂ receptor binding ligands, the tracer-uptake ratio of the striatum-to-frontal cortex or cerebellum during the equilibrium phase provides an estimate of binding potential (Bound/Free = B(max)/K(d)). Our experiment showed that these ratio increased with time after bolus injection of the tracer. Striatum to frontal cortex or cerebellum ratios which were calculated with pooled data (n = 12) at 60 minutes in equilibrium phase showed nearly constant values (C.V. = 12.3% and 13.5%, respectively). Although measuring the striatum to frontal cortex or cerebellum ratios near equilibrium phase by bolus injection of the tracer which are widely used in human SPECT study could not exactly signify the binding potential, those ratios at fixed time after injection would be reliable for semiquantitative index.