Naiker Dineshree V, Catts Stanley V, Catts Vibeke S, Bedi Kuldip S, Bryan-Lluka Lesley J
School of Medicine, The University of Queensland, Brisbane QLD 4072 Australia.
Eur J Pharmacol. 2006 Jul 1;540(1-3):87-90. doi: 10.1016/j.ejphar.2006.04.048. Epub 2006 May 11.
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.
本研究的目的是确定在大鼠中使氟哌啶醇、利培酮和奥氮平达到80%纹状体多巴胺D2受体占有率的抗精神病药物剂量。通过渗透微型泵对Wistar大鼠进行为期7天的处理，分别给予生理盐水（对照组）、氟哌啶醇（0.25和0.5 mg/kg/天）、利培酮（3、5和6 mg/kg/天）和奥氮平（5和10 mg/kg/天）。收集纹状体和小脑组织，并使用3H-雷氯必利测定体内多巴胺D2受体占有率。在11周龄和24周龄大鼠中达到80%多巴胺D2受体占有率所需的剂量分别为：氟哌啶醇0.25 mg/kg/天、利培酮5 mg/kg/天和奥氮平10 mg/kg/天。
