Pardoprunox
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.
At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Pardoprunox hydrochloride) usually boasts enhanced water solubility and stability.
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- CAS No.: 269718-84-5
- Formule: C12H15N3O2
- Masse moléculaire:233.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Other In-stock Forms of Pardoprunox
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
5-HT1A Receptor 6.3 (pEC50) |
D2 Receptor 8 (pEC50) |
D3 Receptor 9.2 (pEC50) |
In Vitro
Pardoprunox (SLV-308) 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 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 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)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 269718-84-5
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Masse moléculaire 233.27
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Formule C12H15N3O2
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SMILES
O=C1OC2=C(N3CCN(C)CC3)C=CC=C2N1
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Synonyms
SLV-308; DU-126891
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. 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. [Content Brief]
[2]. Bronzova J, et al. Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease. Mov Disord. 2010 Apr 30;25(6):738-46. [Content Brief]
[3]. Bétry C, et al. In vivo effects of pardoprunox (SLV308), a partial D?/D? receptor and 5-HT1A receptor agonist, on rat dopamine and serotonin neuronal activity. Synapse. 2011 Oct;65(10):1042-51. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pardoprunox Related Classifications
HY-14958 Related Classifications
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