Pardoprunox - CAS 269718-84-5
Catalog number: 269718-84-5
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
5-HT Receptor | Dopamine Receptor
Pardoprunox, also called as SLV308 or DU-126891, is 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%) that has shown antiparkinsonian potential in animal
Solid powder
7-(4-methylpiperazin-1-yl)-3H-1,3-benzoxazol-2-one2(3H)-benzoxazolone, 7-(4-methyl-1-piperazinyl)-monohydrochloridepardoprunoxSLV-308; SME-308; SLV 308; SME 308; SLV308; SME308
Soluble in DMSO
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -146℃ for long term (months to years).
Shelf Life:
2 years
1.258±0.06 g/cm3
Canonical SMILES:
1.Pardoprunox reverses motor deficits but induces only mild dyskinesia in MPTP-treated common marmosets.
Johnston LC1, Jackson MJ, Rose S, McCreary AC, Jenner P. Mov Disord. 2010 Oct 15;25(13):2059-66. doi: 10.1002/mds.23249.
Long-acting full dopamine D(2) agonists produce less dyskinesia in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated primates and in Parkinson's disease than effective antiparkinsonian doses of levodopa. They do not however, prevent priming for dyskinesia expression on subsequent levodopa exposure. In contrast, the effects of partial D(2) receptor agonists on dyskinesia are unclear. We now examine the ability of the partial D(2) agonist pardoprunox (SLV308) to improve motor function and its propensity to prime for dyskinesia in drug naïve, MPTP-treated common marmosets. Previously, drug naïve, MPTP-treated common marmosets were treated with equivalent doses of either pardoprunox (SLV308) (0.1 mg/kg po), ropinirole (0.18 mg/kg po), or levodopa (10 mg/kg po BID) for 28 days. All treatments induced a similar reduction of motor disability. Dyskinesia induced by levodopa was of greater intensity than that following administration of either pardoprunox (SLV308) or ropinirole.
2.The partial dopamine agonist pardoprunox (SLV308) administered in combination with l-dopa improves efficacy and decreases dyskinesia in MPTP treated common marmosets.
Tayarani-Binazir K1, Jackson MJ, Rose S, McCreary AC, Jenner P. Exp Neurol. 2010 Dec;226(2):320-7. doi: 10.1016/j.expneurol.2010.09.007. Epub 2010 Sep 16.
Dopamine agonist treatment in early Parkinson's disease (PD) induces less dyskinesia than l-dopa. However, once dyskinesia has developed, dopamine agonists administered with l-dopa exacerbate involuntary movements. The dopamine partial D2/D3 agonist pardoprunox reverses motor deficits in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine hydrochloride (MPTP)-treated primates without hyperactivity, indicating that pardoprunox may alleviate dyskinesia without compromising l-dopa's beneficial actions. This study examines a clinical scenario in which pardoprunox was introduced, in an l-dopa sparing strategy, to existing l-dopa treatment in MPTP-treated marmosets previously primed to express dyskinesia. l-Dopa (5-10 mg/kg) produced effects, which were stable over the 13 treatment days, of increased locomotor activity, reversed motor disability and marked dyskinesia. Pardoprunox (SLV308; 0.0125-0.025 mg/kg) plus l-dopa (3-10 mg/kg) administration increased locomotor activity over the same treatment period and initially produced an equivalent reversal of motor disability compared to l-dopa, however this effect was enhanced as treatment progressed.
3.In vivo effects of pardoprunox (SLV308), a partial D₂/D₃ receptor and 5-HT1A receptor agonist, on rat dopamine and serotonin neuronal activity.
Bétry C1, Etiévant A, Lambás-Señas L, McCreary AC, Haddjeri N. Synapse. 2011 Oct;65(10):1042-51. doi: 10.1002/syn.20936. Epub 2011 May 3.
The nonergot ligand pardoprunox (SLV308) is a dopamine (DA) D₂/D₃ and serotonin (5-HT)(1A) receptor agonist and a new candidate for the treatment of Parkinson's disease. We used in vivo electrophysiological paradigm in the rat to assess the effects of pardoprunox on DA neuronal activity in ventral tegmental area (VTA) and substantia nigra pars compacta (SNc) as well as on 5-HT neuronal activity in dorsal raphe nucleus (DRN). In the VTA, pardoprunox (2-20 μg kg⁻¹, i.v.) decreased partially the firing activity of DA neurons. Interestingly, the bursting activity of VTA DA neurons was completely suppressed. This compound both reversed and prevented the inhibition of firing rate induced by the full D₂-like receptor agonist apomorphine, confirming its partial D₂-like receptor agonistic property. Surprisingly in the SNc, pardoprunox (10 μg kg⁻¹, i.v.) either partially or fully suppressed the firing activity in two separate populations of DA neurons.
4.Pardoprunox in early Parkinson's disease: results from 2 large, randomized double-blind trials.
Sampaio C1, Bronzova J, Hauser RA, Lang AE, Rascol O, van de Witte SV, Theeuwes AA; Rembrandt/Vermeer Study Groups. Mov Disord. 2011 Jul;26(8):1464-76. doi: 10.1002/mds.23590. Epub 2011 May 3.
This report presents the results of 2 randomized trials-Rembrandt and Vermeer-on the efficacy and safety of pardoprunox in patients with early Parkinson's disease. Patients with Parkinson's disease with a Unified Parkinson's Disease Rating Scale-Motor score ≥ 10 and modified Hoehn and Yahr stage ≤ 3 were randomized to pardoprunox (fixed doses of 6 mg/day [n = 115] or 12 mg/day [n = 118] or a flexible-dose range of 12-42 mg/day [n = 116]) or placebo (n = 119) in Rembrandt and pardoprunox 12-42 mg/day (n = 108), pramipexole 1.5-4.5 mg/day (n = 116), or placebo (n = 110) in Vermeer. Pardoprunox showed a significant benefit over placebo in the primary efficacy variable, least-square mean change from baseline in Unified Parkinson's Disease Rating Scale-Motor score: Rembrandt-fixed doses of 6 and 12 mg/day, -6.0 and -4.7 points, respectively; flexible-dose 12-42 mg/day, -5.5 points; placebo, -2.9 points; Vermeer-flexible-dose 12-42 mg/day, -4.
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CAS 269718-84-5 Pardoprunox

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