Do antipsychotic drugs and serotonin down regulate [3H]-spiroperidol binding sites in human cortex?
[3H]-Spiroperidol binds at several specific sites in postmortem human prefrontal cortex at 21 degrees C. The overall selectivity of these sites is serotonergic. At 37 degrees C, there is a marked loss of specific [3H]-spiroperidol binding that occurs between 10 and 60 min. This loss of binding is not apparently due to 3H-ligand degeneration or metabolism, or to non-specific binding site degradation. The loss of binding can also be produced by serotonin (5-HT), haloperidol and chlorpromazine but not by prazosin. The rate of the loss of binding is dependent on 3H-ligand concentration and protein concentration. The loss of binding is correlated with a loss of serotonin selective [3H]-spiroperidol binding sites having a KD of approximately 0.04 nM. Therefore antipsychotic compounds and 5-HT appear to down-regulate a subset of antipsychotic binding sites in human prefrontal cortex.
Andorn
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D000293:Adolescent; D000328:Adult; D014150:Antipsychotic Agents / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects; D002090:Butyrophenones / Q000378:metabolism*; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D002746:Chlorpromazine / Q000494:pharmacology; D006220:Haloperidol / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D008875:Middle Aged; D011224:Prazosin / Q000494:pharmacology; D012701:Serotonin / Q000494:pharmacology*; D013134:Spiperone / Q000378:metabolism*
D014150:Antipsychotic Agents; D002090:Butyrophenones; D012701:Serotonin; D013134:Spiperone; D006220:Haloperidol; D002746:Chlorpromazine; D011224:Prazosin