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Vilazodone (EMD 68843; SB 659746A) is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression.
| Targets |
5-HT1A Receptor
|
|---|---|
| ln Vitro |
Vilazodone has an IC50 of 0.5 nM for the SERT and 0.2 nM at the human 5-HT1A receptor. Vilazodone exhibits high affinity (pKi≥9.3) for human recombinant and native tissue 5-HT1A receptors from rats, mice, marmosets, and guinea pigs, and it preferentially binds to the high agonist affinity state of human 5-HT1A receptors.
Vilazodone functions at 5-HT1A receptors as a partial agonist with high efficacy. A single concentration of Vilazodone (100nM) increases basal binding by approximately 70% of that produced by the full 5-HT1A receptor agonist, 8‐OH‐PIPAT, in [35S]GTPγS binding studies in Sf9 cells expressing h5-HT1A receptors.
Vilazodone exhibits potent partial agonistic effects on the 5‐HT1A receptor, as demonstrated by [35S]GTPγS binding studies conducted in rat hippocampal membranes. Its intrinsic activity is 0.61 and its pEC50 is 8.1.
Vilazodone has a potent inhibitory effect on 5‐HT reuptake in the cortex of rats and guinea pigs. Vilazodone has an 8.8 pIC50 to inhibit [3H]5-HT uptake in LLCPK cells that express human SERT[1].
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| ln Vivo |
Vilazodone (intraperitoneal injection; 3 mg/kg ; single dose) causes increases in extracellular 5‐HT in rat frontal cortex (FC) and ventral hippocampal (vHipp) in in vivo microdialysis studies. Maximum increases are seen at 3 mg/kg, where they reach, in the FC and vHipp, 527% and 558% of preinjection baseline values, respectively[2].
Vilazodone (55 mg/kg; single dose; oral gavage) inhibits vocalizations induced by stress in the rat ultrasonic vocalizations test 120 and 210 minutes after the dose[2].
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| References |
|
| Molecular Formula |
C₂₆H₂₇N₅O₂
|
|---|---|
| Molecular Weight |
441.52
|
| Exact Mass |
441.22
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| CAS # |
163521-12-8
|
| Related CAS # |
Vilazodone Hydrochloride; 163521-08-2; Vilazodone-d8; 1794789-93-7; Vilazodone carboxylic acid; 163521-19-5
|
| Appearance |
Powder
|
| SMILES |
C1CN(CCN1CCCCC2=CNC3=C2C=C(C=C3)C#N)C4=CC5=C(C=C4)OC(=C5)C(=O)N
|
| InChi Key |
SGEGOXDYSFKCPT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C26H27N5O2/c27-16-18-4-6-23-22(13-18)19(17-29-23)3-1-2-8-30-9-11-31(12-10-30)21-5-7-24-20(14-21)15-25(33-24)26(28)32/h4-7,13-15,17,29H,1-3,8-12H2,(H2,28,32)
|
| Chemical Name |
5-[4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl]-1-benzofuran-2-carboxamide
|
| Synonyms |
EMD 68843; SB659746A; Vilazodone; EMD68843; EMD-68843
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 75~88 mg/mL (199.3~169.9 mM)
Ethanol: ~14 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2649 mL | 11.3245 mL | 22.6490 mL | |
| 5 mM | 0.4530 mL | 2.2649 mL | 4.5298 mL | |
| 10 mM | 0.2265 mL | 1.1325 mL | 2.2649 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05948579 | Not yet recruiting | Drug: Intervention B Vilazodone Hydrochloride (HCl) Drug: Intervention B Placebo |
Post Traumatic Stress Disorder | U.S. Army Medical Research and Development Command |
August 2023 | Phase 2 |
| NCT05422612 | Recruiting | Drug: Intervention A Placebo Drug: Intervention B Placebo |
Post Traumatic Stress Disorder | U.S. Army Medical Research and Development Command |
November 2, 2023 | Phase 2 |
| NCT02015546 | Completed | Drug: Vilazodone | Major Depressive Disorder (MDD) |
Duke University | December 2012 | Phase 3 |
| NCT02436239 | Completed | Drug: Vilazodone | Major Depressive Disorder | Forest Laboratories | May 2, 2015 | Phase 3 |
| NCT01828515 | Completed | Drug: Vilazodone Drug: Placebo |
Memory Impairment | University of Texas Southwestern Medical Center |
December 2012 | Phase 2 |
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