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MedKoo Cat#: 531230 | Name: Pardoprunox free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pardoprunox, also known as SLV-308; DU-126891; SME-308, is dopamine D2/5-HT1A receptor agonist potentially for the treatment of Parkinson's disease. It was also being investigated for the treatment of depression and anxiety but these indications appear to have been abandoned. 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%). 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.

Chemical Structure

Pardoprunox free base
Pardoprunox free base
CAS#269718-84-5 (free base)

Theoretical Analysis

MedKoo Cat#: 531230

Name: Pardoprunox free base

CAS#: 269718-84-5 (free base)

Chemical Formula: C12H15N3O2

Exact Mass: 233.1164

Molecular Weight: 233.27

Elemental Analysis: C, 61.79; H, 6.48; N, 18.01; O, 13.72

Price and Availability

Size Price Availability Quantity
1g USD 2,450.00 3-4 weeks
2g USD 3,850.00 3-4 weeks
5g USD 5,950.00 3-4 weeks
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Related CAS #
269718-83-4 (HCl) 269718-84-5 (free base)
Synonym
SLV-308; SLV 308; SLV308; DU-126891; SME-308; DU126891; SME308; Pardoprunox; Pardoprunox
IUPAC/Chemical Name
7-(4-methylpiperazin-1-yl)-3H-1,3-benzoxazol-2-one
InChi Key
YVPUUUDAZYFFQT-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H15N3O2/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)
SMILES Code
O=C1OC2=C(N3CCN(C)CC3)C=CC=C2N1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Pardoprunox (SLV-308) is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC50s of 8, 9.2, and 6.3, respectively.
In vitro activity:
SLV308 binds to dopamine D(2), D(3), and D(4) receptors and 5-HT(1) (A) receptors and is a partial agonist at dopamine D(2) and D(3) receptors and a full agonist at serotonin 5-HT(1) (A) receptors. At cloned human dopamine D(2,L) receptors, SLV308 acted as a potent but partial D(2) receptor agonist (pEC(50) = 8.0 and pA(2) = 8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D(3) receptors, SLV308 acted as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA(2) = 9.0). SLV308 acted as a full 5-HT(1) (A) receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT(1) (A) receptors but with low potency (pEC(50) = 6.3). In rat striatal slices SLV308 concentration-dependently attenuated forskolin stimulated accumulation of cAMP, as expected for a dopamine D(2) and D(3) receptor agonist. SLV308 antagonized the inhibitory effect of quinpirole on K(+)-stimulated [(3)H]-dopamine release from rat striatal slices (pA(2) = 8.5). In the same paradigm, SLV308 had antagonist properties in the presence of quinpirole (pA(2) = 8.5), but the partial D(2) agonist terguride had much stronger antagonistic properties. Reference: Synapse. 2006 Dec 15;60(8):599-608. https://pubmed.ncbi.nlm.nih.gov/17001660/
In vivo activity:
This study 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. 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. Finally, in the DRN, pardoprunox (5-40 μg kg⁻¹, i.v.) completely suppressed the firing activity of 5-HT neurons. Moreover, the selective 5-HT(1A) receptor antagonist WAY-100,635 prevented and reversed the effects of pardoprunox. The present study shows that pardoprunox acts in the VTA as a potent partial D₂-like receptor agonist reducing preferentially the burst activity linked to the phasic activity of DA neurons. Reference: Synapse. 2011 Oct;65(10):1042-51. https://pubmed.ncbi.nlm.nih.gov/21446003/

Preparing Stock Solutions

The following data is based on the product molecular weight 233.27 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Glennon JC, Van Scharrenburg G, Ronken E, Hesselink MB, Reinders JH, Van Der Neut M, Long SK, Feenstra RW, McCreary AC. 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. 2006 Dec 15;60(8):599-608. doi: 10.1002/syn.20330. PMID: 17001660. 2. Bétry C, Etiévant A, Lambás-Señas L, McCreary AC, Haddjeri N. In vivo effects of pardoprunox (SLV308), a partial D₂/D₃ receptor and 5-HT1A receptor agonist, on rat dopamine and serotonin neuronal activity. Synapse. 2011 Oct;65(10):1042-51. doi: 10.1002/syn.20936. Epub 2011 May 3. PMID: 21446003. 3. Tayarani-Binazir K, Jackson MJ, Rose S, McCreary AC, Jenner P. The partial dopamine agonist pardoprunox (SLV308) administered in combination with l-dopa improves efficacy and decreases dyskinesia in MPTP treated common marmosets. Exp Neurol. 2010 Dec;226(2):320-7. doi: 10.1016/j.expneurol.2010.09.007. Epub 2010 Sep 16. PMID: 20843474.
In vitro protocol:
1. Glennon JC, Van Scharrenburg G, Ronken E, Hesselink MB, Reinders JH, Van Der Neut M, Long SK, Feenstra RW, McCreary AC. 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. 2006 Dec 15;60(8):599-608. doi: 10.1002/syn.20330. PMID: 17001660.
In vivo protocol:
1. Bétry C, Etiévant A, Lambás-Señas L, McCreary AC, Haddjeri N. In vivo effects of pardoprunox (SLV308), a partial D₂/D₃ receptor and 5-HT1A receptor agonist, on rat dopamine and serotonin neuronal activity. Synapse. 2011 Oct;65(10):1042-51. doi: 10.1002/syn.20936. Epub 2011 May 3. PMID: 21446003. 2. Tayarani-Binazir K, Jackson MJ, Rose S, McCreary AC, Jenner P. The partial dopamine agonist pardoprunox (SLV308) administered in combination with l-dopa improves efficacy and decreases dyskinesia in MPTP treated common marmosets. Exp Neurol. 2010 Dec;226(2):320-7. doi: 10.1016/j.expneurol.2010.09.007. Epub 2010 Sep 16. PMID: 20843474.
1: Al-Kassmy J, Sun C, Huot P. 5-HT1A agonists for levodopa-induced dyskinesia in Parkinson's disease. Neurodegener Dis Manag. 2023 Apr;13(2):101-112. doi: 10.2217/nmt-2022-0039. Epub 2023 May 4. PMID: 37140165. 2: Qureshi AR, Rana AQ, Malik SH, Rizvi SFH, Akhter S, Vannabouathong C, Sarfraz Z, Rana R. Comprehensive Examination of Therapies for Pain in Parkinson's Disease: A Systematic Review and Meta-Analysis. Neuroepidemiology. 2018;51(3-4):190-206. doi: 10.1159/000492221. Epub 2018 Aug 28. PMID: 30153669. 3: Pahwa R, Lyons KE. Treatment of early Parkinson's disease. Curr Opin Neurol. 2014 Aug;27(4):442-9. doi: 10.1097/WCO.0000000000000113. PMID: 24950010. 4: Ye N, Song Z, Zhang A. Dual ligands targeting dopamine D2 and serotonin 5-HT1A receptors as new antipsychotical or anti-Parkinsonian agents. Curr Med Chem. 2014;21(4):437-57. doi: 10.2174/09298673113206660300. PMID: 24164194. 5: Rascol O, Bronzova J, Hauser RA, Lang AE, Sampaio C, Theeuwes A, van de Witte SV. 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. 2012 May;18(4):370-6. doi: 10.1016/j.parkreldis.2011.12.006. Epub 2012 Feb 7. PMID: 22316635. 6: Goetz CG, Stebbins GT, Theeuwes A, Stocchi F, Ferreira JJ, van de Witte S, Bronzova J. Temporal stability of the Unified Dyskinesia Rating Scale. Mov Disord. 2011 Dec;26(14):2556-9. doi: 10.1002/mds.23931. Epub 2011 Sep 13. PMID: 21915907. 7: Sampaio C, Bronzova J, Hauser RA, Lang AE, Rascol O, van de Witte SV, Theeuwes AA; Rembrandt/Vermeer Study Groups. Pardoprunox in early Parkinson's disease: results from 2 large, randomized double-blind trials. Mov Disord. 2011 Jul;26(8):1464-76. doi: 10.1002/mds.23590. Epub 2011 May 3. PMID: 21542016. 8: Bétry C, Etiévant A, Lambás-Señas L, McCreary AC, Haddjeri N. In vivo effects of pardoprunox (SLV308), a partial D₂/D₃ receptor and 5-HT1A receptor agonist, on rat dopamine and serotonin neuronal activity. Synapse. 2011 Oct;65(10):1042-51. doi: 10.1002/syn.20936. Epub 2011 May 3. PMID: 21446003. 9: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2010 Sep;32(7):517-48. doi: 10.1358/mf.2010.32.7.1549223. PMID: 21069103. 10: Tayarani-Binazir K, Jackson MJ, Rose S, McCreary AC, Jenner P. The partial dopamine agonist pardoprunox (SLV308) administered in combination with l-dopa improves efficacy and decreases dyskinesia in MPTP treated common marmosets. Exp Neurol. 2010 Dec;226(2):320-7. doi: 10.1016/j.expneurol.2010.09.007. Epub 2010 Sep 16. PMID: 20843474. 11: Johnston LC, Jackson MJ, Rose S, McCreary AC, Jenner P. Pardoprunox reverses motor deficits but induces only mild dyskinesia in MPTP-treated common marmosets. Mov Disord. 2010 Oct 15;25(13):2059-66. doi: 10.1002/mds.23249. PMID: 20721904. 12: Grosset D, Grosset A. The Movement Disorder Society--14th International Congress of Parkinson's Disease and Movement Disorders. IDrugs. 2010 Aug;13(8):539-42. PMID: 20721824. 13: Jones CA, Johnston LC, Jackson MJ, Smith LA, van Scharrenburg G, Rose S, Jenner PG, McCreary AC. An in vivo pharmacological evaluation of pardoprunox (SLV308)--a novel combined dopamine D(2)/D(3) receptor partial agonist and 5-HT(1A) receptor agonist with efficacy in experimental models of Parkinson's disease. Eur Neuropsychopharmacol. 2010 Aug;20(8):582-93. doi: 10.1016/j.euroneuro.2010.03.001. PMID: 20434890. 14: Bronzova J, Sampaio C, Hauser RA, Lang AE, Rascol O, Theeuwes A, van de Witte SV, van Scharrenburg G; Bruegel Study Group. Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease. Mov Disord. 2010 Apr 30;25(6):738-46. doi: 10.1002/mds.22948. PMID: 20198713. 15: Hauser RA, Bronzova J, Sampaio C, Lang AE, Rascol O, Theeuwes A, van de Witte SV; Pardoprunox Study Group. Safety and tolerability of pardoprunox, a new partial dopamine agonist, in a randomized, controlled study of patients with advanced Parkinson's disease. Eur Neurol. 2009;62(1):40-8. doi: 10.1159/000216839. Epub 2009 Apr 30. PMID: 19407454. 16: Gottwald MD, Aminoff MJ. New frontiers in the pharmacological management of Parkinson's disease. Drugs Today (Barc). 2008 Jul;44(7):531-45. doi: 10.1358/dot.2008.44.7.1217105. PMID: 18806903. 17: Glennon JC, Van Scharrenburg G, Ronken E, Hesselink MB, Reinders JH, Van Der Neut M, Long SK, Feenstra RW, McCreary AC. 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. 2006 Dec 15;60(8):599-608. doi: 10.1002/syn.20330. PMID: 17001660. 18: Wolf WA. SLV-308. Solvay. Curr Opin Investig Drugs. 2003 Jul;4(7):878-82. PMID: 14619412.