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Therapeutic and Diagnostic Agents for Parkinson's Disease

CNS Disorders

  1. Raymond G. Booth1,
  2. John L. Neumeyer2,
  3. Ross J. Baldessarini2

Published Online: 15 SEP 2010

DOI: 10.1002/0471266949.bmc105.pub2

Burger's Medicinal Chemistry and Drug Discovery

Burger's Medicinal Chemistry and Drug Discovery

How to Cite

Booth, R. G., Neumeyer, J. L. and Baldessarini, R. J. 2010. Therapeutic and Diagnostic Agents for Parkinson's Disease. Burger's Medicinal Chemistry and Drug Discovery. 529–568.

Author Information

  1. 1

    University of Florida, Gainesville, FL

  2. 2

    Harvard Medical School, Boston, MA

Publication History

  1. Published Online: 15 SEP 2010


This chapter summarizes the neurobiology of Parkinson's disease and medicinal chemistry relevant to treatment of this neurodegenerative disorder with neuropsychiatric complications. The chapter also surveys basic clinical features of Parkinson's disease, its neuropathophysiology and etiology. Considered are genetic, maturational, metabolic, and environmental contributors to risk for the disease. Pharmacotherapy for Parkinson's disease includes l-dopa to counter cerebral dopamine deficiency, direct dopaminergic agonists, and agents that prolong the actions of l-dopa or dopamine by preventing their metabolism by peripheral aromatic amino acid decarboxylase, catechol-O-methyltransferase, or monoamine oxidase. Additional drugs acting on nondopaminergic systems include muscarinic acetylcholine, adenosine, and l-glutamate antagonists, as well as serotonin (5-hydroxytryptamine) agonists. Agents used to diagnose Parkinson's disease and monitor its progression, include radioactive compounds used to image brain l-dopa and dopamine neurotransporters and dopamine receptors. Finally, potential contributions are considered of medicinal chemistry to improve pharmacotherapy of Parkinson's disease.


  • adenosine antagonist;
  • basal ganglia;
  • COMT inhibitor;
  • decarboxylase inhibitor;
  • dopamine;
  • dopamine agonist;
  • D1 agonist;
  • D2 agonist;
  • ergolines;
  • glutamate antagonist;
  • levodopa;
  • MAO inhibitor;
  • neurodegeneration;
  • MPTP;
  • oxidation;
  • Parkinson's disease;
  • parkinsonism;
  • pramipexole;
  • radioligand;
  • ropinirole;
  • serotonin agonist