Domino E F, Ni L, Zhang H, Kohno Y, Sasa M
Department of Pharmacology, University of Michigan, Ann Arbor 48109, USA.
Jpn J Pharmacol. 1998 Jul;77(3):227-33. doi: 10.1254/jjp.77.227.
The effects of talipexole on functional motor improvement in comparison with contraversive circling were studied in five chronic (5-7 years post MPTP-lesioned) hemiparkinsonian Macaca nemestrina monkeys. Talipexole induced contraversive rotations in a dose of 32 microg/kg for about 1 hr after i.m. injection. Larger doses (56 and 100 microg/kg, i.m.) produced less effect due to sedation. Three different rating scales were used to assess functional improvement, including a clinical parkinsonism rating scale, volitional responses to fruit presentations, and number of significant hand movements. The optimal dose of talipexole was 32 microg/kg, i.m. Functional improvement by talipexole, including clinical parkinsonian rating scales and significant hand movements, as well as contraversive circling in hemiparkinsonian monkeys, confirm that this chronic animal model is useful in preclinical testing of drugs for the treatment of human parkinsonism.
在五只慢性(MPTP损伤后5 - 7年)偏侧帕金森病食蟹猴中,研究了他利克索与对侧旋转相比对功能性运动改善的影响。他利克索经肌肉注射后,剂量为32微克/千克时可诱导对侧旋转约1小时。较大剂量(56和100微克/千克,肌肉注射)由于镇静作用效果较差。使用三种不同的评分量表来评估功能改善情况,包括临床帕金森病评分量表、对水果呈现的自主反应以及明显手部动作的数量。他利克索的最佳剂量为32微克/千克,肌肉注射。他利克索对偏侧帕金森病猴子的功能改善,包括临床帕金森病评分量表和明显手部动作,以及对侧旋转,证实了这种慢性动物模型在治疗人类帕金森病药物的临床前测试中是有用的。