[3H]ketanserin binding in human brain postmortem.
This study aimed at comparing the binding characteristics of [3H]ketanserin, a high-affinity serotonin 2A (5-HT2A) receptor antagonist, in the prefrontal cortex, hippocampus and striatum of human brain post-mortem. The results indicated the presence of a single population of binding sites in all the regions investigated, with no statistical difference in maximum binding capacity (B(max)) or dissociation constant (K(d)) values. The pharmacological profile of [3H]ketanserin binding was consistent with the labeling of the 5-HT2A receptor, since it revealed a competing drug potency ranking of ketanserin = spiperone > clozapine = haloperidol > methysergide > mesulergine > 5-HT. In conclusion, the 5-HT2A receptor, as labeled by [3H]ketanserin, would seem to consist of a homogenous population of binding sites and to be equally distributed in human prefronto-cortical, limbic and extrapyramidal structures.
Marazziti
D
D
Istituto di Psichiatria, Università di Pisa, Roma, Italia. dmarazzipsico.med.unipi.it.
Rossi
A
A
Palego
L
L
Giannaccini
G
G
Naccarato
A
A
Lucacchini
A
A
Cassano
G B
GB
D001344:Autopsy; D001479:Basal Ganglia / Q000378:metabolism*; D001665:Binding Sites; D006624:Hippocampus / Q000378:metabolism*; D006801:Humans; D007650:Ketanserin / Q000378:metabolism*; D017397:Prefrontal Cortex / Q000378:metabolism*; D011869:Radioligand Assay
D007650:Ketanserin