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Baudry M, Martres MP, Schwartz JC. 
“In Vivo Binding of 3H-Pimozide in Mouse Striatum: Effects of Dopamine Agonists and Antagonists”. 
Life Sci.. 1977;21(8):1163-1170.
The effects of dopamine (DA) agonists and antagonists on the striatal binding of pimozide (Janssen) was studied. Male Swiss albino (20-25 g) mice were given 3H-pimozide at 4.33 nmol/kg (specific activity 13 Ci/mmol) i.v. and killed by decapitation at various-intervals. Brains were dissected and different areas examined for retained radioactivity. Striatal homovanillic acid (HVA) was also measured by a standard method. Results About 0,30f 0.002 mg/kg 3H-pimozide was retained in the brain at 30 min with approximately equal concentrations in the cerebellum, the striatum and the cortex, Radioactivity then rapidly disappeared from the cerebellum but remained at its initial level in the striatum until 3 hr and then disappeared slowly, Dis-appearance of 3H from the cortex was intermediate between the cerebellum and striatum. Subsequent experiments were performed with the mice killed 2 hr after administration of 3H - pimozide. Both haloperidol and sulpiride prevented, in a dose-dependent manner, retention of 3H-pimozide in the striatum without affecting cerebellum levels. The ED -50 was 0.07 mg/kg for haloperidol and 22 mg/kg for sulpiride. The ED -50 for the increase in striatal level of HVA was 0.06 mg/kg for haloperidol and 16 mg/kg for sulpiride. L-DOPA and d-amphetamine 1 mg/kg had no effect but apomorphine prevented the retention of 3H - pimozide. Higher doses of d-amphetamine increased the striatal level of 3H-pimozide. Propranolol, clonidine, methysergide, LSD, scopolamine, promethazine, chlordiazepoxide or baclofen had no effect but in morphine-treated mice, 3H-pimozide retention in both striatum and cerebellum was increased.
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