A novel dopamine agonist for the transdermal treatment of Parkinson's disease.
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.
Jenner
Peter
P
Neurodegenerative Diseases Research Centre, Guy's, King's and St Thomas' School of Biomedical Sciences, King's College, London, United Kingdom. peter.jenner@kcl.ac.uk
D000279:Administration, Cutaneous; D000818:Animals; D000978:Antiparkinson Agents / Q000008:administration & dosage / Q000494:pharmacology*; D018491:Dopamine Agonists / Q000008:administration & dosage / Q000494:pharmacology*; D006801:Humans; D017661:Receptors, Presynaptic / Q000187:drug effects; D013237:Stereoisomerism; D013764:Tetrahydronaphthalenes / Q000008:administration & dosage / Q000494:pharmacology*; D013876:Thiophenes / Q000008:administration & dosage / Q000494:pharmacology*
D000978:Antiparkinson Agents; D018491:Dopamine Agonists; D017661:Receptors, Presynaptic; D013764:Tetrahydronaphthalenes; D013876:Thiophenes; C047508:rotigotine