Pardoprunox free base
featured

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

MedKoo CAT#: 531230

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

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.


Chemical Structure

img
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: 233.12
Molecular Weight: 233.271
Elemental Analysis: C, 61.79; H, 6.48; N, 18.01; O, 13.72

Price and Availability

Size Price Availability Quantity
1g USD 2450 3-4 weeks
2g USD 3850 3-4 weeks
5g USD 5950 3-4 weeks
Bulk inquiry

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:
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.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x