163521-08-2
5-[4-[4-(5-Cyanoindol-3-yl)butyl]piperazin-1-yl]benzofuran-2-carboxamide hydrochloride
CAS: 163521-08-2
Molecular Formula: C26H28ClN5O2
163521-08-2 - Names and Identifiers
163521-08-2 - Physico-chemical Properties
| Molecular Formula | C26H28ClN5O2 |
| Molar Mass | 477.98582 |
| Melting Point | 279°C(lit.) |
| Boling Point | 745.1℃ at 760 mmHg |
| Flash Point | 9℃ |
| Solubility | DMSO: soluble20mg/mL, clear |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| Stability | Hygroscopic |
| In vitro study | The IC 50 of Vilazodone binding to human 5-HT1A receptor and SERT were 0.2 nM and 0.5 nM, respectively. Vilazodone showed high affinity (PKI ≥ 9.3) for recombinant human and natural tissue 5-HT1A receptors in rats, guinea pigs, mice, and marmosets. |
| In vivo study | Vilazodone selectively enhances serotonin production in rat prefrontal cortex. In the anxiety rat model of ultrasound vocalization, Vilazodone demonstrated anxiolytic efficacy by behavioral evaluation. A single dose of Vilazodone was also shown to be effective in the forced swim test. Vilazodone(1-10 mg/kg, P. O.) dose-dependently displaces [3 H] DASB(N, n-dimethyl-2-(2-amino-4-cyanophenylthio) in vivo benzylamine) bound to the rat cerebral cortex and hippocampus, suggesting that Vilazodone occupies the serotonin transporter in vivo. In the frontal cortex of freely moving rats, Vilazodone(10 mg/kg, oral) was shown to cause a 2-fold increase in extracellular 5-HT, but no change in noradrenaline or dopamine levels. In rats, Vilazodone affected the stress-enhancing effect of startle at doses higher than 5 mg/kg. At a dose of 10 mg/kg, Vilazodone increased the pressure rise of startle. The effects of Vilazodone(20 mg/kg and 40 mg/kg) inhibited the stress-enhancing effect of startle. In rats, all doses of Vilazodone increased the pressure rise of startle. In the dorsal raphe nucleus of the guinea pig, Vilazodone had no effect on the efflux of 5-HT at 100 nM, but significantly reduced the efflux of serotonin at 1 mM. In the dorsal raphe nucleus of the guinea pig, Vilazodone significantly increased the Half-Life of serotonin reuptake. |
163521-08-2 - Risk and Safety
| Risk Codes | R11 - Highly Flammable R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R39/23/24/25 - |
| Safety Description | S7 - Keep container tightly closed. S16 - Keep away from sources of ignition. S36/37 - Wear suitable protective clothing and gloves. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN1230 - class 3 - PG 2 - Methanol, solution |
| WGK Germany | 3 |
| HS Code | 29329990 |
163521-08-2 - Reference Information
| biological activity | Vilazodone is a combination of serotonin reuptake specific inhibitor (SSRI) and partial agonist of 5-HT1A receptor, which is currently being clinically evaluated for the treatment of depression. |
| Target | Value |
Last Update：2024-04-09 20:49:11
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