Chemistry:Pardoprunox

From HandWiki
Short description: Antiparkinsonian compound researched for the treatment of depression and anxiety disorders
Pardoprunox
Pardoprunox.png
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC12H15N3O2
Molar mass233.271 g·mol−1
3D model (JSmol)

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][1] 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 (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. ↑ 1.0 1.1 1.2 1.3 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". http://clinicaltrials.gov/ct2/results?term=pardoprunox. 
  3. ↑ "Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease". Movement Disorders 25 (6): 738–746. March 2010. doi:10.1002/mds.22948. PMID 20198713. 
  4. ↑ 4.0 4.1 4.2 "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. doi:10.1002/syn.20330. PMID 17001660. 
  5. ↑ "New frontiers in the pharmacological management of Parkinson's disease". Drugs of Today 44 (7): 531–45. July 2008. doi:10.1358/dot.2008.44.7.1217105. PMID 18806903. http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summaryn_pr?p_JournalId=4&p_RefId=1217105. 

Further reading




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