Ex vivo 3H-spiroperidol binding to rat striatum and the inhibitory effects of neuroleptics.
Neuroleptic drugs were given to rats and at different time intervals the animals were decapitated and 3H-spiroperidol binding to the striatal homogenates was determined in vitro. Two hours after an intraperitoneal administration of spiroperidol, perphenazine, haloperidol, chlorpromazine or thioridazine in doses of 0.03-30 mg/kg, 3H-spiroperidol, binding to the striatal homogenates was inhibited dose-dependently with an ID50 value of 0.11, 0.23, 1.1, 3.7 or 9.4 mg/kg, respectively. After a single intramuscular administration of fluphenazine enanthate (10 mg/kg), a long-acting neuroleptic drug, long-lasting inhibitory effect (over 4 weeks) on the binding was also observed. These results indicate that ex vivo 3H-spiroperidol binding method may be useful to measure the duration and the potency of anti-dopaminergic activities of drugs.
D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D002090:Butyrophenones / Q000378:metabolism*; D003342:Corpus Striatum / Q000378:metabolism*; D018492:Dopamine Antagonists; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects; D013134:Spiperone / Q000378:metabolism*; D013997:Time Factors; D014316:Tritium
D014150:Antipsychotic Agents; D002090:Butyrophenones; D018492:Dopamine Antagonists; D011954:Receptors, Dopamine; D014316:Tritium; D013134:Spiperone