Parkinson's disease--opportunities for novel therapeutics to reduce the problems of levodopa therapy

Prog Brain Res. 2008:172:479-94. doi: 10.1016/S0079-6123(08)00923-0.

Abstract

Long-term treatment for Parkinson's disease (PD) with the dopamine-precursor levodopa (l-DOPA) results in the development of motor fluctuations, including involuntary movements, termed l-DOPA-induced dyskinesia (LID). Currently, effective treatments for LID are limited. The neurodegenerative processes underlying PD result in loss of serotonin (5-HT) input from the dorsal raphe nucleus (DRN) to the striatum, but to a lesser extent than loss of dopamine input. l-DOPA may be converted to dopamine in remaining serotonergic neurons and the non-physiological release of dopamine may lead to abnormal dopamine receptor stimulation in the striatopallidal pathways and result in the generation of LID. Suppressing the activity of these 5-HT inputs to the striatum via presynaptic 5-HT(1A) agonists may reduce LID. However, to date, studies with 5-HT(1A) agonists have suggested a reduction in LID, but with worsening PD disability. Postsynaptic 5-HT(2A) and 5-HT(2C) receptors in the striatum may modulate dopamine to reduce LID and the atypical antipsychotic, clozapine is effective at reducing LID without worsening PD. Alternatively, postsynaptic 5-HT(1A), presynaptic 5-HT(1B/1D) receptors and 5-HT(2C) receptors may modulate GABA and glutamate release within other basal ganglia nuclei to reduce LID. Thus, 5-HT ligands can modulate basal ganglia function and hence motor function through several receptor subtypes and locations, with potential therapeutic benefit to the motor complications induced by long-term l-DOPA therapy in PD. Future studies are needed to develop 5-HT selective drugs that can reduce LID without affecting the anti-parkinsonian action of l-DOPA.

Publication types

  • Review

MeSH terms

  • Animals
  • Basal Ganglia / anatomy & histology
  • Basal Ganglia / metabolism
  • Basal Ganglia / pathology
  • Clinical Trials as Topic
  • Disease Models, Animal
  • Dopamine / metabolism
  • Dyskinesia, Drug-Induced / drug therapy
  • Dyskinesia, Drug-Induced / etiology*
  • Dyskinesia, Drug-Induced / pathology
  • Dyskinesia, Drug-Induced / physiopathology
  • Humans
  • Levodopa* / adverse effects
  • Levodopa* / therapeutic use
  • Parkinson Disease / complications*
  • Parkinson Disease / drug therapy*
  • Parkinson Disease / pathology
  • Parkinson Disease / physiopathology
  • Protein Isoforms / metabolism
  • Receptors, Serotonin / metabolism
  • Serotonin / metabolism

Substances

  • Protein Isoforms
  • Receptors, Serotonin
  • Serotonin
  • Levodopa
  • Dopamine