Pardoprunox

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] It was also being investigated for the treatment of depression and anxiety but these indications appear to have been abandoned as well.[1]

Pardoprunox

Clinical data
Routes of administration	Oral
ATC code	none
Legal status
Legal status	In general: uncontrolled
Identifiers
IUPAC name 7-(4-methylpiperazin-1-yl)-3H-1,3-benzoxazol-2-one
CAS Number	269718-84-5
PubChem CID	6918524
ChemSpider	5293721
UNII	5R72CHP32S
CompTox Dashboard (EPA)	DTXSID80949746
ECHA InfoCard	100.206.783
Chemical and physical data
Formula	C12H15N3O2
Molar mass	233.271 g·mol^−1
3D model (JSmol)	Interactive image
SMILES Cl.O=C2Oc1c(cccc1N2)N3CCN(C)CC3

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
• Pimavanserin

References

1. Wolf WA (July 2003). "SLV-308. Solvay". Current Opinion in Investigational Drugs. 4 (7): 878–82. PMID 14619412.
2. "Search of: pardoprunox - List Results - ClinicalTrials.gov".
3. Bronzova J, Sampaio C, Hauser RA, et al. (March 2010). "Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease". Movement Disorders. 25 (6): 738–746. doi:10.1002/mds.22948. PMID 20198713.
4. Glennon JC, Van Scharrenburg G, Ronken E, et al. (December 2006). "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. doi:10.1002/syn.20330. PMID 17001660.
5. Gottwald MD, Aminoff MJ (July 2008). "New frontiers in the pharmacological management of Parkinson's disease". Drugs of Today. 44 (7): 531–45. doi:10.1358/dot.2008.44.7.1217105. PMID 18806903.

Further reading

• Hauser RA, Bronzova J, Sampaio C, et al. (2009). "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. doi:10.1159/000216839. PMID 19407454.
• Bronzova J, Sampaio C, Hauser RA, et al. (March 2010). "Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease". Movement Disorders. 25 (6): 738–746. doi:10.1002/mds.22948. PMID 20198713.