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[3H]ketanserin binding in human brain postmortem.

D Marazziti·A Rossi·L Palego·G Giannaccini·A Naccarato·A Lucacchini·G B Cassano
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Abstract

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.

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AutopsyBasal GangliaBinding SitesHippocampusHumansKetanserinPrefrontal CortexRadioligand AssayJournal Article

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D Marazziti, A Rossi, L Palego, G Giannaccini, A Naccarato, A Lucacchini, G B Cassano. 1997. [3H]ketanserin binding in human brain postmortem.. https://doi.org/10.1023/a%3A1027366413289

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