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Pardoprunox

From Wikipedia, the free encyclopedia
Antiparkinsonian compound researched for the treatment of depression and anxiety disorders
Pharmaceutical compound
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
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
ECHA InfoCard100.206.783Edit 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 nameSLV-308) is anantiparkinsoniandrug developed bySolvay for the treatment ofParkinson's disease that reachedphase IIIclinical trials before being discontinued.[1][2][3][1] It was also being investigated for the treatment ofdepression andanxiety but these indications appear to have been abandoned as well.[1]

Pardoprunox acts as aD2 (pKi = 8.1) andD3 receptor (pKi = 8.6)partial agonist (IA = 50% and 67%, respectively) and5-HT1A receptor (pKi = 8.5)full agonist (IA = 100%).[1][4] It also binds toD4 (pKi = 7.8),α1-adrenergic (pKi = 7.8),α2-adrenergic (pKi = 7.4), and5-HT7 receptors (pKi = 7.2) with loweraffinity.[1][4] Relative to other dopaminergic antiparkinsonian agents, pardoprunox is thought to have significantly less of a propensity for inducing certainside effects likedyskinesia andpsychosis.[4][5]

See also

[edit]

References

[edit]
  1. ^abcdWolf 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. ^abcGlennon 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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Dopaminergics
DAprecursors
DA receptoragonists
MAO-Binhibitors
COMTinhibitors
AAADinhibitors
Anticholinergics
Others
α1
Agonists
Antagonists
α2
Agonists
Antagonists
β
Agonists
Antagonists
D1-like
Agonists
PAMs
Antagonists
D2-like
Agonists
Antagonists
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Simple piperazines
(no additional rings)
Phenylpiperazines
Benzylpiperazines
Diphenylalkylpiperazines
(benzhydrylalkylpiperazines)
Pyrimidinylpiperazines
Pyridinylpiperazines
Benzo(iso)thiazolylpiperazines
Tricyclics
(piperazine attached via side chain)
Others/Uncategorized


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