Pardoprunox

Pardoprunox

Pardoprunox
Systematic (IUPAC) name
7-(4-methylpiperazin-1-yl)-3H-1,3-benzoxazol-2-one
Clinical data
Legal status
  • Uncontrolled
Routes Oral
Identifiers
CAS number
ATC code None
PubChem
ChemSpider
UNII  YesY
Chemical data
Formula C12H15N3O2 
Mol. mass 269.73 g/mol

Pardoprunox (SLV-308) is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease and as of March 2010 is in Phase III clinical trials.[1][2][3] It was also being investigated for the treatment of depression and anxiety but these indications appear to have been abandoned.[1]

Pardoprunox acts as a D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%).[1][4] It also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 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

References

  1. ^ a b c d Wolf WA (July 2003). "SLV-308. Solvay". Current Opinion in Investigational Drugs (London, England : 2000) 4 (7): 878–82.  
  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 : Official Journal of the Movement Disorder Society 25 (6): NA–NA.  
  4. ^ a b c 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.  
  5. ^ Gottwald MD, Aminoff MJ (July 2008). "New frontiers in the pharmacological management of Parkinson's disease". Drugs of Today (Barcelona, Spain : 1998) 44 (7): 531–45.  

Further reading