Ex vivo 3H-spiroperidol binding to rat striatum and the inhibitory effects of neuroleptics.

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Abstract
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 i.p. 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 i.m. administration of fluphenazine enanthate (10 mg/kg), a long-acting neuroleptic drug, long-lasting inhibitory effect (> 4 wk) on the binding was observed. Ex vivo 3H-spiroperidol binding method may be useful to measure the duration and the potency of antidopaminergic activities of drugs.