Molecular Formula | C12H16ClN3O2 |
Molar Mass | 269.72734 |
Solubility | DMSO : 150 mg/mL (556.11 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) |
Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
Use | Pardoprunox (SLV-308) hydrochloride are dopamine receptor D2, D3 partial agonist and 5-HT1A agonist with pEC50 of 8, 9.2 and 6.3 respectively. |
In vitro study | Pardoprunox (SLV-308) hydrochloride acts as a potent but partial D2 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 D3 receptors, Pardoprunox hydrochloride acts 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). 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 (pEC 50 =6.3). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.707 ml | 18.537 ml | 37.074 ml |
5 mM | 0.741 ml | 3.707 ml | 7.415 ml |
10 mM | 0.371 ml | 1.854 ml | 3.707 ml |
5 mM | 0.074 ml | 0.371 ml | 0.741 ml |
biological activity | pardoplunox hydrozolide (DU-126891, SME-308) is a potent partial agonist of the dopamine D2 receptor, corresponding to a pEC50 value of 8.0, which is also a partial agonist that induces [35S] gtpγs binding, corresponding to a pEC50 value of 9.2, and an agonist of serotonin 5-HT1A receptor, the pEC50 value was 6.3. |
Target | Value |
[ (Cell-free assay) | 9.2(pEC50) |
D2 receptor (Cell-free assay) | 8.0(pEC50) |
5-HT1A receptor (Cell-free assay) | 6.3(pEC50) |