This study aimed at comparing the binding characteristics of [H-3]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 [H-3]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 [H-3]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.

[H-3]ketanserin binding in human brain postmortem

ROSSI, ALESSANDRA;PALEGO, LIONELLA;GIANNACCINI, GINO;LUCACCHINI, ANTONIO;
1997

Abstract

This study aimed at comparing the binding characteristics of [H-3]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 [H-3]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 [H-3]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; Rossi, Alessandra; Palego, Lionella; Giannaccini, Gino; Naccarato, ANTONIO GIUSEPPE; Lucacchini, Antonio; Cassano, Gb
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/176568
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