[Stimulation by cerulein--an analog of the octapeptide cholecystokinin--of 3H-spiroperidol binding after the long-term administration of neuroleptics].
It has been established in experiments on white male rats that prolonged administration (twice a day for 14 days) of haloperidol (0.25 mg/kg) and pyreneperone (0.25 mg/kg) resulted in the reduced interaction between 3H-spiroperidol and low affinity binding sites for apomorphine in subcortical structures, whereas 3H-spiroperidol binding with high affinity binding sites for apomorphine increased both in the frontal cortex and subcortical structures of the forebrain. After prolonged administration of neuroleptics the displacing effect of cerulein, an analog of cholecystokinin octapeptide, was replaced by the stimulant action on 3H-spiroperidol binding. It is assumed that increased interaction between 3H-spiroperidol and high affinity binding sites for apomorphine on dopamine2- and serotonin2-receptors underlies the antipsychotic action of neuroleptics after their prolonged administration. Cholecystokinin octapeptide is a necessary factor for realization of this action of neuroleptics.
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D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D001058:Apomorphine / Q000031:analogs & derivatives / Q000494:pharmacology; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002090:Butyrophenones / Q000378:metabolism*; D002108:Ceruletide / Q000494:pharmacology*; D004347:Drug Interactions; D008297:Male; D051379:Mice; D013134:Spiperone / Q000378:metabolism*; D013268:Stimulation, Chemical; D013997:Time Factors; D014316:Tritium
D014150:Antipsychotic Agents; D002090:Butyrophenones; D014316:Tritium; D013134:Spiperone; C009074:N-n-propylnorapomorphine; D002108:Ceruletide; D001058:Apomorphine
Stimuliatsiia tseruleinom--analogom oktapeptida kholetsistokinina--sviazyvaniia 3H-spiroperidola posle dlitel'nogo vvedeniia neĭroleptikov.