MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 317119 | Name: Pardoprunox HCl
Featured New

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 HCl
Pardoprunox HCl
CAS#269718-83-4 (HCl)

Theoretical Analysis

MedKoo Cat#: 317119

Name: Pardoprunox HCl

CAS#: 269718-83-4 (HCl)

Chemical Formula: C12H16ClN3O2

Exact Mass: 0.0000

Molecular Weight: 269.73

Elemental Analysis: C, 53.44; H, 5.98; Cl, 13.14; N, 15.58; O, 11.86

Price and Availability

Size Price Availability Quantity
10mg USD 90.00 Ready to ship
25mg USD 150.00 Ready to ship
50mg USD 250.00 Ready to ship
100mg USD 450.00 Ready to ship
200mg USD 750.00 Ready to ship
500mg USD 1,250.00 Ready to ship
1g USD 2,150.00 2 weeks
2g USD 3,850.00 2 weeks
5g USD 6,950.00 2 weeks
Show More
Bulk Inquiry
Buy Now
Add to Cart
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
Appearance
Pale mauve 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, 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
More Info
Related CAS# 269718-83-4 (HCl); 269718-84-5 (free base).
Biological target:
Pardoprunox (SLV-308) hydrochloride 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:
In the present study, the in vitro characterization of the nonergot ligand SLV308 (7-[4-methyl-1-piperazinyl]-2(3H)benzoxazolonemonohydrochloride) is described. 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. In conclusion, SLV308 combines high potency partial agonism at dopamine D(2) and D(3) receptors with full efficacy low potency serotonin 5-HT(1) (A) receptor agonism and is worthy of profiling in in vivo models of Parkinson's disease. Reference: Synapse. 2006 Dec 15;60(8):599-608. https://pubmed.ncbi.nlm.nih.gov/17001660/
In vivo activity:
The present study focussed on the in vivo pharmacological and therapeutic characterisation of the novel D(2/3) receptor partial agonist and full 5-HT(1A) receptor agonist pardoprunox (SLV308; 7-[4-methyl-1-piperazinyl]-2(3H)-benzoxazolone monochloride). Pardoprunox induced contralateral turning behaviour in rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra pars compacta (SNpc) (MED=0.03mg/kg; po). In 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated common marmosets, pardoprunox dose-dependently increased locomotor activity (MED=0.03mg/kg; po) and decreased motor disability (MED=0.03mg/kg; po). The effects of pardoprunox were reversed by the D(2) antagonist sulpiride. In contrast pardoprunox attenuated novelty-induced locomotor activity (MED=0.01mg/kg; po), (+)-amphetamine-induced hyperlocomotion (MED=0.3mg/kg; po) and apomorphine-induced climbing (MED=0.6mg/kg; po) in rodents. Pardoprunox also induced 5-HT(1A) receptor-mediated behaviours, including flat body posture and lower lip retraction (MED=0.3mg/kg; po) and these were reversed by the 5-HT(1A) receptor antagonist WAY100635. Collectively, these findings demonstrate that pardoprunox possesses dopamine D2/3 partial agonist effects, 5-HT1A agonist effects and reduces parkinsonism in animal models. Reference: Eur Neuropsychopharmacol. 2010 Aug;20(8):582-93. https://pubmed.ncbi.nlm.nih.gov/20434890/
Solvent mg/mL mM
Solubility
DMSO 5.0 18.50
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 269.73 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. 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.
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. 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.
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.