Pardoprunox Explained

Pardoprunox (INN) (code name SLV-308) is an antiparkinsonian drug developed by Solvay for the treatment of Parkinson's disease that reached phase III clinical trials before being discontinued.^{[1] [2] [3]} http://adisinsight.springer.com/drugs/800014329 It was also being investigated for the treatment of depression and anxiety but these indications appear to have been abandoned as well.^[1]

Pardoprunox acts as a D₂ (pK_i = 8.1) and D₃ receptor (pK_i = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT_1A receptor (pK_i = 8.5) full agonist (IA = 100%).^{[1] [4]} It also binds to D₄ (pK_i = 7.8), α₁-adrenergic (pK_i = 7.8), α₂-adrenergic (pK_i = 7.4), and 5-HT₇ receptors (pK_i = 7.2) with lower affinity.^{[1] [4]} Relative to other dopaminergic antiparkinsonian agents, pardoprunox is thought to have significantly less of a propensity for inducing certain side effects like dyskinesia and psychosis.^{[4] [5]}

See also

• Aripiprazole
• Bifeprunox

Further reading

• Hauser RA, Bronzova J, Sampaio C, etal . Safety and tolerability of pardoprunox, a new partial dopamine agonist, in a randomized, controlled study of patients with advanced Parkinson's disease . European Neurology . 62 . 1 . 40–8 . 2009 . 19407454 . 10.1159/000216839 . 39669742 .
• Bronzova J, Sampaio C, Hauser RA, etal . Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease . Movement Disorders . 25. 6. 738–746. March 2010 . 20198713 . 10.1002/mds.22948 . 206241386 .

Notes and References

1. Wolf WA . SLV-308. Solvay . Current Opinion in Investigational Drugs . 4 . 7 . 878–82 . July 2003 . 14619412 .
2. Web site: Search of: pardoprunox - List Results - ClinicalTrials.gov .
3. Bronzova J, Sampaio C, Hauser RA, etal . Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease . Movement Disorders . 25. 6. 738–746. March 2010 . 20198713 . 10.1002/mds.22948 . 206241386 .
4. Glennon JC, Van Scharrenburg G, Ronken E, etal . In vitro characterization of SLV308 (7-[4-methyl-1-piperazinyl]-2(3H)-benzoxazolone, monohydrochloride): a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist . Synapse . 60 . 8 . 599–608 . December 2006 . 17001660 . 10.1002/syn.20330 . 27227349 .
5. Gottwald MD, Aminoff MJ . New frontiers in the pharmacological management of Parkinson's disease . Drugs of Today . 44 . 7 . 531–45 . July 2008 . 18806903 . 10.1358/dot.2008.44.7.1217105 .