Vilazodone Hydrochloride

SKU: orb1300955

Description

Vilazodone Hydrochloride is a combined serotonin partial agonist and reuptake inhibitor (SPARI) used in major depressive disorder research. It serves as a pharmacological tool for studying 5-HT1A receptor function and SSRI mechanisms in both in vitro binding assays and in vivo behavioral models of depression.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 163521-08-2
• MW: 477.99
• Purity: >99.99% (May vary between batches)
• Formula: C₂₆H₂₇N₅O₂·HCl
• SMILES: Cl.NC(=O)c1cc2cc(ccc2o1)N1CCN(CCCCc2c[nH]c3ccc(cc23)C#N)CC1
• Target: 5-HT Receptor,Serotonin Transporter
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.18 mM);DMSO:45 mg/mL (94.14 mM)

Bioactivity

• In Vivo:
  Vilazodone selectively enhances serotonergic output in the prefrontal cortex of rats. Vilazodone demonstrates anxiolytic efficacy through Behavioral evaluations in the ultrasonic vocalization model of anxiety in rats. Vilazodone also shows efficacy but at a single dose only in the forced swim test (a putative model of depression). Vilazodone (1-10 mg/kg p.o.) dose-dependently displaces in vivo [3H]DASB (N,N-dimethyl-2-(2-amino-4-cyanophenylthio)benzylamine) binding from rat cortex and hippocampus, indicating that vilazodone occupies 5-HT transporters in vivo. Vilazodone (10 mg/kg p.o.) is demonstrated to cause a 2-fold increase in extracellular 5-HT but no change in noradrenaline or dopamine levels in frontal cortex of freely moving rats. Vilazodone affects stress potentiation of startle at doses above 5 mg/kg in rats. Vilazodone increases stress elevation of startle at 10 mg/kg in rats. Vilazodone (20 and 40 mg/kg) blocked stress potentiation of startle in rats. Vilazodone increases stress elevation of startle at all doses in rats. vilazodone has no effect on 5-HT efflux at 100 nM but significantly decreases 5-HT efflux at 1 mM in the guinea-pig dorsal raphe nucleus. Vilazodone significantly increases the re-uptake half life for 5-HT in the guinea-pig dorsal raphe nucleus.
• In Vitro:
  Vilazodone demonstrates an IC50 of 0.2 nM at the human 5-HT1A receptor and 0.5 nM for the SERT. Vilazodone displays high affinity (pKi ≥ 9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT1A receptors.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5-HT Receptor, 5-HT1A, 5HT Receptor, 5HTReceptor, 5-HTT, 5-hydroxytryptamine Receptor, inhibit, Inhibitor, EMD 68843, EMD-68843, EMD68843, Vilazodone, Vilazodone HCl, Vilazodone Hydrochloride, SERT, Serotonin Receptor, Serotonin Transporter, SerotoninTransporter, SSRI, SB659746A, SLC6A4

Compound Identifiers

PubChem CID

6918313