A dopamine D2 and D3 receptor partial agonist and 5-HT1A agonist
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Pardoprunox (hydrochloride)

Item No. 23456

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-(4-methyl-1-piperazinyl)-2(3H)-benzoxazolone, monohydrochloride
CAS Number
269718-83-4
Synonyms
  • DU-126891
  • SLV 308
Molecular Formula
C12H15N3O2 • HCl
Formula Weight
269.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 5 mg/mlEthanol: 0.1 mg/mlPBS (pH 7.2): 5 mg/ml
λmax
219 nm
SMILES
CN1CCN(C2=CC=CC(N3)=C2OC3=O)CC1.Cl
InChi Code
InChI=1S/C12H15N3O2.ClH/c1-14-5-7-15(8-6-14)10-4-2-3-9-11(10)17-12(16)13-9;/h2-4H,5-8H2,1H3,(H,13,16);1H
InChi Key
NQRIKTDKFHAOKC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $41

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    5 mg

    $178

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    10 mg

    $312

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    25 mg

    $680

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    Product Description

    Pardoprunox is a partial agonist of dopamine D2 and D3 receptors (EC50s = 10 and 0.63 nM, respectively) and a full agonist of the serotonin (5-HT) receptor subtype 5-HT1A (EC50 = 501 nM) in radioligand binding assays.1 It is selective for dopamine D2 and D3 and 5-HT1A receptors over a panel of neurotransmitter receptors (Kis = >1,000 nM). Pardoprunox reduces the accumulation of cAMP induced by forskolin (Item No. 11018) in a concentration-dependent manner and blocks quinpirole-induced inhibition of dopamine release (pA2 = 8.5) in rat striatal slices. Pardoprunox increases contralateral turning behavior in a 6-OHDA rat model of Parkinson’s disease (ED50 = 0.03 mg/kg).2 It also reduces hyperlocomotion induced by amphetamine (Item Nos. 14204 | ISO60188) and induces 5-HT1A-mediated flat body posturing and lower lip retraction in rats. Pardoprunox (0.01-0.3 mg/kg) increases locomotor activity in a marmoset model of Parkinson’s disease induced by MPTP in a dose-dependent manner. Formulations containing pardoprunox are under clinical investigation for the treatment of Parkinson’s disease-associated motor fluctuations.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Glennon, J.C., Van Scharrenburg, G., Ronken, E., et al. 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 (2006).

    2. Jones, C.A., Johnston, L.C., Jackson, M.J., et al. An in vivo pharmacological evaluation of pardoprunox (SLV308)—A novel combined dopamine D2/D3 receptor partial agonist and 5-HT1A receptor agonist with efficacy in experimental models of Parkinson’s disease. Eur. Neuropsychopharmacol. 20(8), 582-593 (2010).

    3. Rascol, O., Brozova, J., Hauser, R.A., et al. Pardoprunox as adjunct therapy to levodopa in patients with Parkinson’s disease experiencing motor fluctuations: Results of a double-blind, randomized, placebo-controlled, trial. Parkinsonism Relat. Disord. 18(4), 370-376 (2012).