Vilazodone Hydrochloride (CAS 163521-12-8) is the hydrochloride salt form of vilazodone, a small‑molecule antidepressant approved by the U.S. Food and Drug Administration for the treatment of major depressive disorder (MDD) in adults.
Vilazodone Hydrochloride is a novel antidepressant with a unique dual mechanism of action: high‑affinity inhibition of the serotonin transporter (SERT, IC₅₀ = 0.5 nM) and partial agonism at the 5‑HT₁A receptor (IC₅₀ = 0.2 nM, intrinsic activity ~60–70%). As the active pharmaceutical ingredient in Viibryd®, Vilazodone Hydrochloride represents a significant advance in the pharmacological treatment of major depressive disorder, offering a differentiated mechanism from conventional SSRIs. Vilazodone Hydrochloride exhibits high selectivity for SERT and 5‑HT₁A over norepinephrine and dopamine transporters, providing a targeted serotonergic profile. In analytical and quality control contexts, Vilazodone Hydrochloride serves as the primary reference standard for analytical method development, method validation (AMV), and quality control (QC) applications for Abbreviated New Drug Applications (ANDA). The compound’s well‑characterized pharmacological profile makes Vilazodone Hydrochloride an essential reference material for research into serotonin pharmacology, depression therapeutics, and the development of novel antidepressant agents.
Product Parameters
Parameter
Specification
Product Name
Vilazodone Hydrochloride
CAS Number
163521-12-8
Molecular Formula
C₂₆H₂₇N₅O₂
Molecular Weight
441.52g/mol
Appearance
Light yellow to off-white powder
Melting Point
203–205°C
Boiling Point
745.1±60.0°C (Predicted)
Storage Condition
Powder: –20°C for 3 years
Indication
This drug is a dual-action agent with both serotonin (HT) 1A partial agonist and selective serotonin reuptake inhibitor (SSRI) properties, representing the first indoolalkylamine-class antidepressant indicated for the treatment of adult patients with major depressive disorder (MDD).
Drug Interaction
Vilazolone is primarily metabolized via the CYP3A4 pathway; therefore, concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole) may increase its plasma concentrations, necessitating a corresponding reduction in dosage. Concurrent administration with CYP3A4 inducers may impair its efficacy. Given vilazolone's mechanism of action, adverse effects, and potential toxicity to 5-HT, coadministration with other Chemicalbook drugs that may affect the 5-HTergic neurotransmitter system (e.g., trypantan, tramadol) increases the risk of serotonin syndrome and neuroleptic malignant syndrome (NMS) and should be used with caution. Concurrent use with nonsteroidal anti-inflammatory drugs (NSAIDs), aspirin, or warfarin may elevate the risk of abnormal bleeding. Additionally, vilazolone must not be administered concomitantly with monoamine oxidase inhibitors (MAOIs); MAOI drugs are contraindicated for at least 14 days prior to or after vilazolone administration.
Bioactivity
Vilazodone (EMD-68843, SB-659746A) is a novel antidepressant with selective 5-HT reuptake inhibition and partial 5-HT1A receptor agonistic activity. Its binding affinity for 5-HT reuptake sites is higher than that for norepinephrine and dopamine sites.
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