163521-12-8
Vilazodone
CAS: 163521-12-8
Molecular Formula: C26H27N5O2
163521-12-8 - Names and Identifiers
163521-12-8 - Physico-chemical Properties
| Molecular Formula | C26H27N5O2 |
| Molar Mass | 441.52 |
| Density | 1.34±0.1 g/cm3(Predicted) |
| Melting Point | 203-205°C |
| Boling Point | 745.1±60.0 °C(Predicted) |
| Solubility | DMSO (Slightly)), Methanol (Slightly) |
| Appearance | Solid |
| Color | Pale Yellow to Beige |
| pKa | 15.98±0.30(Predicted) |
| Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| Stability | Very Hygroscopic |
| Use | Vilazodone is an inhibitor of ST (serotonin transporter and uptake) (IC50=0.5 nM) and SR-1A activator (partial agonist) (IC50=0.2 nM; IA = ~60-70%). |
| In vitro study | Vilazodone shows an IC 50 of 0.2 nM at the human 5-HT 1 A receptor and 0.5 nM for the SERT. Vilazodone preferentially binds to the high agonist affinity state of human 5-HT 1 Areceptors, and it displays high affinity (pK i ≥9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT 1A receptors.Vilazodone acts as a high efficacy partial agonist at 5-HT 1 Areceptors. In [ 35 S]GTPγS binding studies in Sf9 cells expressing h5-HT 1 Areceptors, a single concentration of Vilazodone (100nM) increases basal binding by approximately 70% of that produced by the full 5-HT 1 Areceptor agonist, 8‐OH‐PIPAT. In [ 35 S]GTPγS binding studies in rat hippocampal membranes, Vilazodone acts as a potent 5‐HT 1A receptor partial agonist with a pEC 50 of 8.1 and an intrinsic activity of 0.61. Vilazodone acts as a potent 5‐HT reuptake inhibitor in rat and guinea pig cortex. In LLCPK cells expressing human SERT, whereby vilazodone inhibits [ 3 H]5‐HT uptake with a pIC 50 of 8.8. |
| In vivo study | Vilazodone (intraperitoneal injection; 3 mg/kg ; single dose) produces increases in extracellular levels of 5‐HT in both the frontal cortex (FC) and ventral hippocampus (vHipp) of rats in vivomicrodialysis studies. Maximum increases are observed at 3 mg/kg and reaches 527% and 558% of preinjection baseline values in the FC and vHipp, respectively. Vilazodone (oral gavage ;55 mg/kg ; single dose) inhibits stress‐induced vocalizations in the rat ultrasonic vocalizations test at 120 and 210 min post dose. |
163521-12-8 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.265 ml | 11.325 ml | 22.649 ml |
| 5 mM | 0.453 ml | 2.265 ml | 4.53 ml |
| 10 mM | 0.226 ml | 1.132 ml | 2.265 ml |
| 5 mM | 0.045 ml | 0.226 ml | 0.453 ml |
Last Update：2024-01-02 23:10:35
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