Table 1

Comparison of radioligands for imaging of 5-HTT in humans

Properties[123I]β-CIT SPECT[11C](+)McN5652 PET[11C]DASB PET[123I]ADAM SPECT
SelectivityNonselective, near 1:1 affinity for 5-HTT to DAT22,23Likely selective 10:1 to 100:1 affinity for 5-HTT over NET24,25Highly selective 1000:1 affinity for 5-HTT over NET or DAT* 26,27Highly selective 1000:1 affinity for 5-HTT over NET or DAT28,29
Displaceability of specific bindingIncomplete30,31In most, but not all, reports19,32,33Highly displaceable26,27,34,35Highly displaceable28,29,36
ReversibilityGood37,38Not adequate to adequate, depending on region18,19,39Adequate in midbrain, good to very good in other regions20,21,40Adequate in midbrain36,41
Brain uptakeAdequate37,38Good19,39Very good20,21,40Adequate36,41
Specific binding to free and nonspecific binding ratioGoodNot adequate in most regions, adequate in thalamus39,42Adequate to very good20,21Not adequate in most regions; adequate in midbrain36,41
Reliability of 5-HTT BPNot measuredModest32Very good to excellent34,43Most regions reasonable41
5-HTT BP measurability in multiple regionsBrainstem only37,38Measurable in thalamus,39 not measurable in cortex19Yes20,21Measurable in midbrain; unclear for other regions36,41
  • * [11C]DASB is also highly selective for 5-HTT over several other targets tested in vitro.

  • For humans (radiotracer performance differs across species.)

  • Depending on brain region.