[3H]Ketanserin Binding in Human Brain Postmortem |
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| Authors: | Marazziti Donatella Rossi Alessandra Palego Lionella Giannaccini Gino Naccarato Antonio Lucacchini Antonio Cassano Giovanni B |
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| Institution: | (1) Istituto di Psichiatria, Università di Pisa, via Roma 67, I-56100 Pisa, Italia;(2) Istituto Policattedra di Discipline Biologiche, Università di Pisa, via Roma 67, I-56100 Pisa, Italia;(3) Istituto di Anatomia Patologica, Università di Pisa, via Roma 67, I-56100 Pisa, Italia |
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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 (Bmax) or dissociation constant (Kd) 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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| Keywords: | Serotonin serotonin 2A receptors [3H]ketanserin human brain prefrontal cortex hippocampus striatum |
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