To assess binding potential in humans, a simple blood test now evaluates the binding affinity of platelets for 11C-PBR28 [35]. 11C-PBR28 [35]
In humans, it has been used to compare MAO-A binding potential in smokers and nonsmokers [7]; however, a rigorous kinetic modeling study in humans has never been performed.
Based on previous findings of increased µ-opioid receptor binding potential in met/met individuals, we would expect an increased analgesic effect of short acting opioids in met/met individuals compared to val/val.
A recent study reported a 26% lower serotonin transporter binding potential in the amygdalae of depressed medication-free patients with bipolar disorder [ 10].
The extension of the PET study of the SPS patient, showing a reduced 11C-FMZ binding potential in limbic structures, supports the concept that the GABAergic system in the amygdala region is affected by the disease, and this is consistent with a significant reduction in GABA-A receptor binding observed in patients with panic disorder and other anxiety-related disorders [14].
PG patients demonstrated a greater reduction in binding potential in the ventral striatum during gambling compared with control subjects, reflecting greater dopaminergic release.
However, a previous PET study reported that [18 F]-altanserin binding potential in several cortical regions, including the prefrontal cortex, was negatively related to the drive for thinness in patients with AN [ 82].
We obtained arterial blood samples for kinetic data analysis and found that the compound had a differential distribution in brain regions, with the highest binding potentials in the frontal and temporal cortices, intermediate binding potential in the thalamus, and low binding potentials in the striatum, hypothalamus, and brainstem.
Finally, with regard to binding potential in the brain, we assumed that equilibrium or near-equilibrium binding conditions existed in the brain at the time of peak brain uptake.
Therefore, to investigate if higher affinity of [18F]NS14490 in vitro translates into higher binding potential in vivo, the radiosynthesis of [18F]NS14490 was optimized and automated to obtain the radiotracer in quantities allowing dynamic PET studies in piglets.
