Vilazodone-d₈ hydrochloride

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].
Vilazodone shows an IC₅₀ of 0.2 nM at the human 5-HT₁A receptor and 0.5 nM for the SERT. Vilazodone preferentially binds to the high agonist affinity state of human 5-HT₁A receptors, 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-HT₁A receptors. In [³⁵S]GTPγS binding studies in Sf9 cells expressing h5-HT₁A receptors, 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 rat hippocampal membranes, Vilazodone acts as a potent 5‐HT_1A receptor partial agonist with a pEC₅₀ 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 [³H]5‐HT uptake with a pIC₅₀ of 8.8^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.