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Pardoprunox

From Wikipedia, the free encyclopedia

Pardoprunox
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • 7-(4-methylpiperazin-1-yl)-3H-1,3-benzoxazol-2-one
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
ECHA InfoCard100.206.783 Edit this at Wikidata
Chemical and physical data
FormulaC12H15N3O2
Molar mass233.271 g·mol−1
3D model (JSmol)
  • Cl.O=C2Oc1c(cccc1N2)N3CCN(C)CC3

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]

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Transcription

See also

References

  1. ^ a b c d 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. S2CID 206241386.
  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. doi:10.1002/syn.20330. PMID 17001660. S2CID 27227349.
  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


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This page was last edited on 29 April 2022, at 15:52
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