Description
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.
Product information
CAS Number: 269718-83-4
Molecular Weight: 269.73
Formula: C12H16ClN3O2
Synonym:
SLV-308 hydrochloride
DU-126891 hydrochloride
Chemical Name: 7-(4-methylpiperazin-1-yl)-2,3-dihydro-1,3-benzoxazol-2-one; chlorohydrogen
Smiles: Cl.CN1CCN(CC1)C1C=CC=C2NC(=O)OC2=1
InChiKey: NQRIKTDKFHAOKC-UHFFFAOYSA-N
InChi: 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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 150 mg/mL (556.11 mM; Need ultrasonic). H2O : < 0.1 mg/mL (insoluble).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Pardoprunox (SLV-308) hydrochloride acts as a potent but partial D2 receptor agonist (pEC50= 8.0 and pA2=8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D3 receptors, Pardoprunox hydrochloride acts as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC50=9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA2=9.0). Pardoprunox hydrochloride acts as a full 5-HT1A receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT1A receptors but with low potency (pEC50=6.3).
References:
- Glennon JC, et al. 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.
- Jones CA, et al. 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):582-593.
Products are for research use only. Not for human use.
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