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 DAT (22), (23)Likely selective 10:1 to 100:1 affinity for 5-HTT over NET (24), (25)Highly selective 1000:1 affinity for 5-HTT over NET or DAT* (26), (27)Highly selective 1000:1 affinity for 5-HTT over NET or DAT (28), (29)
Displaceability of specific bindingIncomplete (30), (31)In most, but not all, reports (19), (32), (33)Highly displaceable (26), (27), (34), (35)Highly displaceable (28), (29), (36)
ReversibilityGood (37), (38)Not adequate to adequate, depending on region (18), (19), (39)Adequate in midbrain, good to very good in other regions (20), (21), (40)Adequate in midbrain (36), (41)
Brain uptakeAdequate (37), (38)Good (19), (39)Very good (20), (21), (40)Adequate (36), (41)
Specific binding to free and nonspecific binding ratioGoodNot adequate in most regions, adequate in thalamus (39), (42)Adequate to very good (20), (21)Not adequate in most regions; adequate in midbrain (36), (41)
Reliability of 5-HTT BPNot measuredModest (32)Very good to excellent (34), (43)Most regions reasonable (41)
5-HTT BP measurability in multiple regionsBrainstem only (37), (38)Measurable in thalamus, (39) not measurable in cortex (19)Yes (20), (21)Measurable in midbrain; unclear for other regions (36), (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.