Pardoprunox HCl
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MedKoo CAT#: 317119

CAS#: 269718-83-4 (HCl)

Description: 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.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 90 Same day
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 750 Same day
500mg USD 1250 Same day
1g USD 2150 2 Weeks
2g USD 3850 2 Weeks
5g USD 6950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-07-10. Prices are subject to change without notice.

Pardoprunox HCl, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 317119
Name: Pardoprunox HCl
CAS#: 269718-83-4 (HCl)
Chemical Formula: C12H16ClN3O2
Exact Mass:
Molecular Weight: 269.729
Elemental Analysis: C, 53.44; H, 5.98; Cl, 13.14; N, 15.58; O, 11.86


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 HCl.

IUPAC/Chemical Name: 7-(4-methylpiperazin-1-yl)-3H-1,3-benzoxazol-2-one hydrochloride

InChi Key: NQRIKTDKFHAOKC-UHFFFAOYSA-N

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

SMILES Code: O=C1OC2=C(N3CCN(C)CC3)C=CC=C2N1.[H]Cl


Technical Data

Appearance:
White to off-white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

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, not in water

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


Additional Information

Related CAS#
269718-83-4 (HCl);
269718-84-5 (free base).


References

1: Pahwa R, Lyons KE. Treatment of early Parkinson's disease. Curr Opin Neurol. 2014 Aug;27(4):442-9. doi: 10.1097/WCO.0000000000000113. Review. PubMed PMID: 24950010.

2: 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. Review. PubMed PMID: 24164194.

3: 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. PubMed PMID: 22316635.

4: 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. PubMed PMID: 21915907.

5: 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. PubMed PMID: 21542016.

6: 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. PubMed PMID: 21446003.

7: 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. PubMed PMID: 21069103.

8: 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. PubMed PMID: 20843474.

9: 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. PubMed PMID: 20721904.

10: 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. PubMed PMID: 20721824.

11: 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. PubMed PMID: 20434890.

12: 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. PubMed PMID: 20198713.

13: 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. PubMed PMID: 19407454.

14: 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. Review. PubMed PMID: 18806903.

15: 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. PubMed PMID: 17001660.

16: Wolf WA. SLV-308. Solvay. Curr Opin Investig Drugs. 2003 Jul;4(7):878-82. Review. PubMed PMID: 14619412.