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)
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Reversibility | Very good with peak in cortex between 10 and 30 min (107), (110) |
Brain uptake | High (106), (107), (109) |
Specific binding to free and nonspecific binding ratio | Very good; binding potential approximately 2 to 3 in age range18–40 yr (89), (107), (110) |
Reliability of 5-HT2A BP | Excellent (116) |
Metabolites | Radioactive metabolites unable to cross blood–brain barrier (117) |