Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat.

Dineshree V Naiker, Stanley V Catts, Vibeke S Catts, Kuldip S Bedi, Lesley J Bryan-Lluka

School of Medicine, The University of Queensland, Brisbane QLD 4072 Australia.

European journal of pharmacology 2006 Jul 1

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The purpose of the present study was to determine antipsychotic doses that achieve 80% striatal dopamine D2-receptor occupancy for haloperidol, risperidone and olanzapine in rats. Wistar rats were treated with normal saline vehicle (controls), haloperidol (0.25 and 0.5 mg/kg/day), risperidone (3, 5 and 6 mg/kg/day) and olanzapine (5 and 10 mg/kg/day) for 7 days via osmotic minipumps. Striatal and cerebellar tissue were collected and in vivo dopamine D2-receptor occupancies were determined using 3H-raclopride. The doses required to achieve dopamine D2-receptor occupancy of 80% in 11- and 24-week old rats were: haloperidol 0.25 mg/kg/day, risperidone 5 mg/kg/day and olanzapine 10 mg/kg/day.

Citation

Dineshree V Naiker, Stanley V Catts, Vibeke S Catts, Kuldip S Bedi, Lesley J Bryan-Lluka. Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat. European journal of pharmacology. 2006 Jul 1;540(1-3):87-90