A novel dopamine agonist for the transdermal treatment of Parkinson's disease
A novel dopamine agonist for the transdermal treatment of Parkinson's disease
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DOI：
10.1212/wnl.65.2_suppl_1.s3
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发表时间：
2005-07-26
期刊：
影响因子：
9.9
通讯作者：
Jenner, P
中科院分区：
文献类型：
--
作者：
Jenner, P
罗替戈汀是一种非麦角、对映体选择性、D3/D2/D1多巴胺(DA)激动剂，在帕金森病(PD)的经典模型中有效，包括保留的小鼠、6-羟基多巴胺损毁的大鼠和MPTP治疗的灵长类动物。口服后有效，但清除率高，作用时间较短。然而，罗替戈汀对6-羟基多巴胺损伤的大鼠和MPTP治疗的猴子经皮给药后也有效，两者的作用时间都明显延长。罗替戈汀的药理特性表明，它具有构成控制帕金森病运动症状的经皮治疗的基础所必需的特征。
Rotigotine is a non-ergot, enantio-selective, D3/D2/D1 dopamine (DA) agonist drug that is effective in classical models of Parkinson's disease (PD), including the reserpinised mouse, the 6-hydroxydopamine-lesioned rat, and the MPTP-treated primate. It is active after oral administration but shows high clearance and a relatively short duration of effect. However, rotigotine is also effective after transdermal application in 6-hydroxydopamine-lesioned rats and MPTP-treated monkeys, in both of which the duration of effect is markedly enhanced. The pharmacologic properties of rotigotine suggest that it has the characteristics necessary to form the basis of a transdermal treatment for the control of motor symptoms of PD.