Table 3

Properties of [18F] Setoperone

Properties[18F] Setoperone
Selectivity and displaceability of specific binding
  • – 100:1 greater affinity for 5-HT2A receptors over 5-HT2C receptors, and a 1:10 to 1:50 greater affinity of 5-HT2A receptors over D2 receptors. (111) Since D2 receptors are 10-fold less dense in human cortex (82) (84), (112) the combined relative effects of affinity and density correspond to an estimate that at least 99% of the specific binding signal in cortex is attributable to 5-HT2A receptors.

  • – No effect of the D2 antagonist amisulpride on [18F] setoperone binding in human cortex (113)

  • – 5-HT2 antagonists fully block specific binding in animal and human cortex (106), (107), (114), (115)

  • – Not selective in striatum where D2 receptor density is high (107)

ReversibilityVery good with peak in cortex between 10 and 30 min (107), (110)
Brain uptakeHigh (106), (107), (109)
Specific binding to free and nonspecific binding ratioVery good; binding potential approximately 2 to 3 in age range18–40 yr (89), (107), (110)
Reliability of 5-HT2A BPExcellent (116)
MetabolitesRadioactive metabolites unable to cross blood–brain barrier (117)